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PI3K
PI3K製品
- All (135)
- PI3K阻害剤 (126)
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- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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| S1105 | LY294002 | LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓ を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。 |
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| S2767 | 3-Methyladenine (3-MA) | 3-Methyladenine (3-MA)は、HeLa細胞におけるVps34およびPI3Kγに対する選択的PI3K阻害剤であり、IC50はそれぞれ25 μMと60 μMです。クラスI PI3Kを一貫して阻害する一方、クラスIII PI3Kの抑制は一時的であり、autophagosome形成も阻害します。溶液は不安定なため、使用直前に調製する必要があります。 |
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| S1009 | Dactolisib (BEZ235) | Dactolisib (BEZ235, NVP-BEZ235)は、ATP競合的なデュアルPI3KおよびmTOR阻害剤であり、p110α/γ/δ/βおよびmTOR(p70S6K)に対し、それぞれ細胞を含まないアッセイでIC50が4 nM /5 nM /7 nM /75 nM /6 nMです。3T3TopBP1-ER細胞においてATRをIC50 21 nMで阻害します。Dactolisibはautophagyを誘導し、HIV-1の複製を抑制します。フェーズ2。 |
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| S1065 | Pictilisib (GDC-0941) | Pictilisib (GDC-0941, RG7321) は、PI3Kα/δ の強力な阻害剤で、無細胞アッセイでは IC50 が 3 nM であり、p110β (11 倍) および p110γ (25 倍) に対しては控えめな選択性を示します。Pictilisib (GDC-0941) は autophagy および apoptosis を誘導します。フェーズ 2。 |
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| S2758 | Wortmannin (SL-2052) | Wortmanninは、初めて記述されたPI3K阻害剤で、細胞を含まないアッセイでのIC50は3 nMであり、PI3Kファミリー内での選択性はほとんどありません。Wortmanninは、autophagosomeの形成を阻害し、細胞を含まないアッセイでIC50が16 nMおよび150 nMでDNA-PK/ATMを強力に阻害します。Wortmanninはまた、PLK1活性も阻害します。 |
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| S2638 | NU7441 (KU-57788) | NU7441 (KU-57788) は、IC50が14 nMの非常に強力で選択的なDNA-PK阻害剤であり、セルリーアッセイにおいてmTORとPI3Kをそれぞれ1.7 μMと5 μMのIC50で阻害します。Cas9を介したDNA切断後、NHEJの頻度を減少させ、HDRの速度を増加させます。 |
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| S2226 | CAL-101 (Idelalisib) | Idelalisib (CAL-101)は、セルフリーアッセイにおいて2.5 nMのIC50を持つ選択的p110δ阻害剤であり、p110α/β/γよりも40〜300倍、C2β、hVPS34、DNA-PK、mTORよりも400〜4000倍高いp110δ選択性を示します。Idelalisibはまた、autophagyを刺激します。 |
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| S2247 | Buparlisib (BKM120) | Buparlisib (BKM120, NVP-BKM120) は、細胞を使用しないアッセイでそれぞれ 52 nM/166 nM/116 nM/262 nM の IC50 を持つ、p110α/β/δ/γ の選択的 PI3K 阻害剤です。VPS34、mTOR、DNAPK に対する効力は低下しており、PI4Kβ に対する活性はほとんどありません。Buparlisib はアポトーシスを誘導します。第2相。 |
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| S2814 | Alpelisib (BYL719) | アルペリシブ (Alpelisib (BYL719)) はPI3Kβ/γ/δ に対する影響が最小限の、強力かつ選択的な PI3Kα 阻害剤(無細胞アッセイで IC50 = 5 nM) です。 臨床フェーズ2。 |
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| S1038 | PI-103 | PI-103 は、無細胞アッセイにおいて IC50 が 2 nM/3 nM/3 nM/15 nM の p110α/β/δ/γ を標的とするマルチ PI3K 阻害剤で、mTOR/DNA-PK に対しては IC50 が 30 nM/23 nM と効力は低い。PI-103 はマウス T 細胞リンパ腫で apoptosis を誘導する。 |
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| S1169 | TGX-221 | TGX-221は、細胞を含まないアッセイで5 nMのIC50を持つp110β特異的阻害剤であり、p110αよりも1000倍p110βに対して選択的です。 |
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| S1072 | ZSTK474 | ZSTK474は、細胞を含まないアッセイで、主にPI3KδであるクラスI PI3Kアイソフォームを37 nMのIC50で阻害します。フェーズ1/2。 |
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| S2893 | NU7026 | NU7026 (LY293646) は、細胞フリーアッセイにおいてIC50が0.23 µMの強力なDNA-PK阻害剤であり、PI3Kに対しては60倍の選択性を示し、ATMおよびATRの両方に対しては不活性です。NU7026はG2/M細胞周期停止とアポトーシスを促進します。 |
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| S2658 | Omipalisib (GSK2126458) | Omipalisib (GSK2126458, GSK458) は、p110α/β/δ/γ および mTORC1/2 の高選択的かつ強力な阻害剤であり、セル-フリーアッセイにおけるKi値はそれぞれ0.019 nM/0.13 nM/0.024 nM/0.06 nM、および0.18 nM/0.3 nMです。Omipalisib はautophagyを誘導します。フェーズ1。 |
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| S2802 | Copanlisib (BAY 80-6946) | Copanlisibは、PI3Kα/β/γ/δのセル・フリーアッセイにおいて、それぞれ0.5、3.7、6.4、0.7 nMのIC50を持つ強力なパンクラスI PI3Kです。フェーズ3。本製品は溶解度が低く、動物実験には使用できますが、細胞実験には慎重にお選びください。 |
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| S2636 | A66 | A66は、無細胞アッセイにおいてIC50が32 nMである強力かつ特異的なp110α阻害剤であり、他のクラスI PI3Kアイソフォームと比較してp110αに対する100倍以上の選択性を示します。 |
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| S7865 | 740 Y-P (PDGFR 740Y-P) | 740 Y-P (PDGFR 740Y-P, 740YPDGFR) is a cell-permeable phosphopeptide activator of PI3K. | ||
| S2391 | Quercetin (Sophoretin) | 野菜、果物、ワインに含まれる天然フラボノイドであるQuercetinは、組換えSIRT1の刺激剤であり、IC50が2.4-5.4 µMのPI3K阻害剤でもあります。Quercetinはmitophagy、apoptosis、および防御的autophagyを誘導します。フェーズ4。 |
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| S2743 | PF-04691502 | PF-04691502（PF4691502）は、ATP競合的なPI3K(α/β/δ/γ)/mTORデュアル阻害剤であり、セルフリーアッセイにおいてKi値が1.8 nM/2.1 nM/1.6 nM/1.9 nMおよび16 nMですが、Vps34、AKT、PDK1、p70S6K、MEK、ERK、p38、またはJNKに対してはほとんど活性がありません。PF-04691502はapoptosisを誘導します。フェーズ2。 |
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| S7028 | IPI-145 (Duvelisib) | Duvelisib (IPI-145, INK1197) は、新規かつ選択的なPI3K δ/γ阻害剤であり、セル-フリーアッセイにおけるKiおよびIC50は23 pM/243 pMおよび1 nM/50 nMで、他のプロテインキナーゼよりもPI3K δ/γに対して高い選択性を示します。フェーズ3。 |
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| S1205 | PIK-75 HCl | PIK-75 HClは、p110α阻害剤であり、IC50は5.8 nM（p110βよりも200倍強力）、Ser773のアイソフォーム特異的変異体を持ち、また無細胞アッセイではDNA-PKをIC50 2 nMで強力に阻害します。 |
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| S7682 | SAR405 | SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells. |
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| S1268 | IC-87114 | IC-87114は、無細胞アッセイにおいてIC50が0.5 µMの選択的PI3Kδ阻害剤であり、PI3Kγよりも58倍、PI3Kα/βよりも100倍以上選択性が高いです。 |
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| S2298 | Fisetin | Fisetin（フィセチン）は、強力なsirtuin活性化化合物（STAC）であり、sirtuinsを調節する薬剤です。 |
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| S1410 | AS-605240 | AS-605240は、細胞を含まないアッセイにおいて、PI3Kδ/βおよびPI3KαよりもPI3Kγに対してそれぞれ30倍および7.5倍以上選択的であり、PI3Kγを8 nMのIC50で選択的に阻害します。 |
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| S7103 | Taselisib (GDC 0032) | Taselisib (GDC 0032, RG7604)は、強力な次世代βアイソフォーム温存PI3K阻害剤であり、PI3Kα/δ/γを標的とし、Ki値は0.29 nM/0.12 nM/0.97 nMで、PI3Kβに対して10倍以上の選択性を示します。 | ||
| S1362 | Rigosertib (ON-01910) | Rigosertib (ON-01910) は、無細胞アッセイにおいてIC50が9 nMの非ATP競争的PLK1阻害剤です。Plk2に対して30倍高い選択性を示し、Plk3には活性がありません。RigosertibはPI3K/Akt経路を阻害し、酸化的ストレスシグナルを活性化します。Rigosertibは様々な癌細胞でapoptosisを誘導します。現在フェーズ3です。 |
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| S2759 | Fimepinostat (CUDC-907) | CUDC-907は、PI3KαとHDAC1/2/3/10に対するデュアルPI3KおよびHDAC阻害剤であり、それぞれ19 nMと1.7 nM/5 nM/1.8 nM/2.8 nMのIC50を示します。CUDC-907は、乳がん細胞において細胞周期停止とapoptosisを誘導します。第1相。 |
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| S7980 | VPS34-IN1 | Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy. |
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| S2696 | Apitolisib (GDC-0980) | Apitolisib (GDC-0980, RG7422, GNE 390) は、クラスI PI3K の強力な阻害剤であり、セルリーアッセイにおいてPI3Kα/β/δ/γ に対するIC50 はそれぞれ5 nM/27 nM/7 nM/14 nM です。また、mTOR 阻害剤でもあり、セルリーアッセイにおけるKi は17 nM で、他のPIKKファミリーキナーゼに対して高い選択性を示します。Apitolisib は、膵臓癌細胞においてAutophagy とApoptosis を同時に活性化します。現在、第2相臨床試験中です。 |
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| S1187 | PIK-90 | PIK-90は、PI3Kα/γ/δ阻害剤であり、それぞれ11 nM/18 nM/58 nMのIC50を持ち、PI3Kβには効力が劣ります。 |
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| S2628 | Gedatolisib (PKI-587) | Gedatolisib (PF-05212384, PKI-587) は、PI3Kα、PI3Kγ、mTORの強力なデュアル阻害剤であり、それぞれセルアッセイでIC50が0.4 nM、5.4 nM、1.6 nMでした。フェーズ2。 |
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| S8330 | Eganelisib (IPI-549) | Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM. | ||
| S1462 | AZD6482 | AZD6482 (KIN-193)は、PI3Kβ阻害剤であり、細胞を含まないアッセイにおいて、PI3Kδ、PI3Kα、およびPI3KγよりもPI3Kβに対して8倍、87倍、109倍選択的であり、IC50は10 nMです。フェーズ1。 |
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| S7683 | PIK-III | PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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| S7356 | HS-173 | HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. |
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| S2671 | AS-252424 | AS-252424は、新規かつ強力なPI3Kγ阻害剤であり、セルフリーアッセイにおいてIC50は30 nMであり、PI3Kαと比較してPI3Kγに対する選択性は30倍高く、PI3Kδ/βに対する阻害活性は低い。 |
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| S7694 | AZD8186 | AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1. | ||
| S8002 | GSK2636771 | GSK2636771は、PI3Kα/PI3Kγに対して900倍以上、PI3Kδに対して10倍以上の選択性を持つ、強力で経口投与可能かつ選択的なPI3Kβ阻害剤です。PTEN欠損細胞株に感受性を示します。 |
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| S1219 | YM201636 | YM201636は、33 nMのIC50を持つ選択的なPIKfyve阻害剤であり、p110αには効力が低く、Fabl（酵母オーソログ）には不感応です。YM-201636は、autophagyの誘導を介して肝臓がんの増殖を抑制します。 |
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| S7016 | VS-5584 (SB2343) | VS-5584 (SB2343)は、強力で選択的なデュアルPI3K/mTOR阻害剤で、mTOR、PI3Kα/β/δ/γに対してそれぞれIC50値が3.4 nMおよび2.6-21 nMです。第1相。 |
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| S7645 | Pilaralisib (XL147) | Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2. |
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| S1360 | GSK1059615 | GSK1059615は、PI3Kα/β/δ/γ（可逆的）およびmTORのデュアル阻害剤であり、それぞれ0.4 nM/0.6 nM/2 nM/5 nMおよび12 nMのIC50を示します。フェーズ1。 |
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| S7018 | CZC24832 | CZC24832は、PI3Kγを27 nMのIC50で阻害する初の選択的阻害剤であり、PI3Kβに対して10倍、PI3KαおよびPI3Kδに対して100倍以上の選択性を示します。 |
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| S1352 | TG100-115 | TG100-115は、PI3Kγ/δ阻害剤であり、IC50は83 nM/235 nMで、PI3Kα/βにはほとんど影響を与えません。フェーズ1/2。 |
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| S7646 | Voxtalisib (XL765) | Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
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| S2749 | BGT226 (NVP-BGT226) maleate | BGT226 (NVP-BGT226)は、IC50が4 nM/63 nM/38 nMのPI3Kα/β/γに対する新規クラスI PI3K/mTOR阻害剤です。臨床第1/2相。 |
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| S8322 | Samotolisib (LY3023414) | LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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| S1118 | XL147 analogue | XL147 analogue (SAR245408)は、細胞を含まないアッセイにおいてIC50が39 nM/36 nM/23 nMのPI3Kα/δ/γに対する選択的かつ可逆的なクラスI PI3K inhibitorであり、PI3Kβに対しては効力が劣ります。XL147 analogueはapoptosisを誘導します。第1/2相。 |
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| S2681 | AS-604850 | AS-604850は、選択的ATP競合的PI3Kγ阻害剤であり、IC50は250 nMです。PI3Kδ/βに対するPI3Kγの選択性は80倍以上であり、PI3Kαに対するPI3Kγの選択性は18倍です。 |
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| S8045 | KU-0060648 | KU-0060648は、DNA-PKおよびPI3Kα、PI3Kβ、PI3Kδのデュアル阻害剤であり、それぞれのIC50は8.6 nM、4 nM、0.5 nM、0.1 nMです。PI3Kγに対する阻害は少なく、IC50は0.59 μMです。 |
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| S8674 | GO-203 TFA | GO-203 is a D-amino acid cell-penetrating peptide inhibitor of MUC1-C dimerization and thereby its oncogenic function. | ||
| S8596 | Autophinib | Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro. | ||
| S2347 | Quercetin Dihydrate | リンゴ、タマネギ、ベリー、赤ワインなど、さまざまな植物性食品に含まれるポリフェノール性フラボノイドであるQuercetin (Sophoretin)は、神経系および抗がん効果のために多くの異なる文化で利用されています。天然のフラボノイドであるQuercetin (dihydrate)は、組換えSIRT1の刺激剤であり、PI3K γ、PI3K δ、PI3K βに対してそれぞれ2.4 μM、3.0 μM、5.4 μMのIC50値を持つPI3K阻害剤です。 |
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| S8456 | VPS34 inhibitor 1 (Compound 19) | VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. |
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| S8194 | umbralisib (TGR-1202) | Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. | ||
| S1523 | Voxtalisib (XL765) Analogue | Voxtalisib (SAR245409, XL765) Analogue は、mTOR/PI3K のデュアルインヒビターであり、主に p110γ に対して IC50 9 nM です。DNA-PK および mTOR も阻害します。第 1/2 相。 |
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| S2739 | PKI-402 | PKI-402は、PI3Kα/β/γ/δおよびmTORをそれぞれ2 nM/7 nM/16 nM/14 nMおよび3 nMのIC50で標的とする強力なデュアルpan-PI3K/mTOR阻害剤です。PI3Kα変異体E545KおよびH1047Rにも強力です。 | ||
| S8668 | GDC-0077 (Inavolisib) | Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3. | ||
| S7813 | AMG319 | AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. | ||
| S8738 | Bimiralisib (PQR309) | Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets. | ||
| S7937 | Nemiralisib | Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). | ||
| S8132 | Deguelin | Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor. | ||
| S2699 | CH5132799 | CH5132799（MEN1611、PA799）は、クラスIのPI3Ksを阻害し、特にPI3KαをIC50 14 nMで阻害します。PI3Kβδγに対しては効果が低いですが、PIK3CA変異細胞株には感受性を示します。第1相。 |
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| S8163 | Paxalisib (GDC-0084) | Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR. | ||
| S8581 | Serabelisib (TAK-117) | Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. | ||
| S2227 | PIK-294 | PIK-294は、p110δに対する高選択的阻害剤であり、IC50は10 nMで、それぞれPI3Kα/β/γに対して1000倍、49倍、16倍効力が低い。 |
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| S2870 | TG100713 | TG100713は、PI3Kγ、PI3Kδ、PI3Kα、PI3Kβに対するパンPI3K阻害剤であり、それぞれのIC50は50 nM、24 nM、165 nM、215 nMです。 |
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| S9190 | Oroxin B | Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment. | ||
| S3238 | Resibufogenin | Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. | ||
| S8589 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. | ||
| S7798 | GNE-317 | GNE-317 is a potent, brain-penetrant PI3K inhibitor. | ||
| S7966 | AZD8835 | AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). | ||
| S3220 | Trigonelline | Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells. | ||
| S6541 | MTX-211 | MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase. | ||
| S8157 | GDC-0326 | GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. | ||
| E2384 | (E)-Akt inhibitor-IV | (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic. | ||
| S3785 | Notoginsenoside R1 | Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways. | ||
| S7623 | PI-3065 | PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members. | ||
| S8693 | Selective PI3Kδ Inhibitor 1 (compound 7n) | Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. | ||
| E0785 | YS-49 | YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors. | ||
| S2682 | CAY10505 | CAY10505は、AS-252424の脱ヒドロキシ体であり、PI3Kγ阻害剤であり、IC50は33 nMです。 |
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| S3294 | Demethyl-Coclaurine | Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes. | ||
| S3296 | Hispidulin | Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. | ||
| E8308New | Alpelisib hydrochloride | Alpelisib hydrochloride is a potent and selective inhibitor of PI3Kα with an IC50 of 0.005 μM, 1.2 μM, 0.29 μM, 0.25 μM for p110α, p110β, p110δ, p110γ, respectively. It exhibits good efficacy in inhibiting the growth of PI3Ka driven tumors and can be used in cancer research. | ||
| S0817 | SKI-V | SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. | ||
| S8560 | Seletalisib (UCB-5857) | Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). | ||
| S8752 | leniolisib (CDZ 173) | Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. | ||
| S5978 | Gallein | Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain. | ||
| S5818 | acalisib (GS-9820) | Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. | ||
| S6885 | Ailanthone | Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. | ||
| S7675 | PF-4989216 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. | ||
| S6516 | GNE-477 | GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. | ||
| S6517 | GNE-493 | GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. | ||
| S2207 | PIK-293 | PIK-293はPI3K阻害剤であり、主にPI3Kδに対してIC50が0.24 μMで、PI3Kα/β/γに対してそれぞれ500倍、100倍、50倍効果が低い。 |
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| E5875New | LY294002 hydrochloride | LY294002 hydrochloride is a potent and specific inhibitor of PI3K with an IC50 of 0.5 μM, 0.97 μM, and 0.57 μM for P110α, P110β, P110δ, respectively. It also acts as a direct blocker of L-type Ca2+ channel with IC50 of 20 µM. | ||
| E2947 | Recilisib | Recilisib (ON01210, EX-RAD) is a radioprotectant that activates the activity of AKT and PI3K in cells. It has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. | ||
| E1076New | Linperlisib | リンペルリシブは、特許WO 2015055071 A1の化合物10から抽出された強力で経口投与可能な選択的PI3Kδ阻害剤であり、IC50は6.4 nMである。 | ||
| S4572 | Homosalate | Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways. | ||
| E4683 | PI3K/AKT-IN-1 | PI3K/AKT-IN-1 is a dual-acting inhibitor of PI3K/AKT pathway with an IC50 of 6.99 µM, 4.01 µM, and 3.36 µM, for PI3Kδ, PI3Kγ and AKT-1 respectively. It also induces S-phase cell cycle arrest, caspase-3-dependent apoptosis, exhibiting strong potential against breast cancer and leukemia. | ||
| S3224 | Cinobufagin | Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. | ||
| S7938 | GSK2292767 | GSK2292767 is a potent and selective PI3Kδ inhibitor. | ||
| S5554 | Lanatoside C | Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways. | ||
| E2375 | PI3K/mTOR Inhibitor-2 | PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity. | ||
| S3243 | Zeaxanthin | Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM. | ||
| S0947 | Cafestol | Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60. | ||
| E4605New | Copanlisib dihydrochloride | Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a selective and potent inhibitor of pan-class I PI3K. It significantly inhibits the catalytic activity of class I PI3K isoforms α, β, γ, and δ with IC50 of 0.5, 3.7, 6.4, and 0.7 nM, respectively. BAY 80-6946 exhibits potent antitumor activity in multiple cell-line–derived and patient-derived xenograft tumor models. | ||
| E1609New | NVP-CLR457 | NVP-CLR457 is an orally active, potent, and balanced inhibitor of pan-class I PI3K. NVP-CLR457 exhibits IC50 values of 12 ± 1.5 nM, 8.3 ± 1.0 nM, 8.3 ± 2.0 nM, 230 ± 31 nM, for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ. It shows a clear dose-dependent PK/PD/efficacy relationship and demonstrates antitumor activity. | ||
| E4864 | Pentamidine | Pentamidine (MP-601205) is an aromatic diamidine drug, an antagonist of TLR4.It also inhibits PI3K/AKT signaling pathway and reduce the expression of MMP-2 and MMP-9. It exhibits anti- protozoal, anti-inflammatory, and anti-tumor activities and is used as an agent for treating African trypanosomiasis, antimony resistant leishmaniasis and Pneumocystis carinii pneumonia. | ||
| E2823 | PIK-108 | PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor. | ||
| E0020 | Lupenone | Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway. | ||
| E4765New | TYM-3-98 | TYM-3-98 is a selective inhibitor of PI3Kδ with an IC50 of 7.1 nM. It blocks the PI3Kδ/AKT signaling pathway, induces apoptosis in B-cell lymphomas, and effectively suppresses xenograft tumor growth in vivo. | ||
| E1815 | Tersolisib (STX-478) | Tersolisib (STX-478) is a highly potent, mutant-selective, allosteric inhibitor of PI3Kα, that selectively targets prevalent mutant forms of PI3Kα. It demonstrates strong efficacy against common PI3Kα helical- and kinase-domain mutations, including the H1047R variant, with an IC50 value of 9.4 nmol/L. STX-478 exhibits 14-fold greater selectivity for mutant PI3Kα over the wild-type form. It spares metabolic dysfunction and improves therapeutic response in PI3Kα-Mutant Xenografts. | ||
| E2366 | IHMT-PI3Kδ-372 | IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay | ||
| S8672 | Tenalisib | Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. | ||
| S3309 | Solasodine | Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21. | ||
| S9054 | Pectolinarin | Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway. | ||
| S8948 | SRX3207 | SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. | ||
| E5809 | Dactolisib Tosylate | Dactolisib Tosylate (BEZ235 Tosylate, NVP-BEZ 235 Tosylate) is an imidazo[4,5-c]quinoline derivative and dual inhibitor of PI3K/mTOR with IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. It blocks mTORC1/mTORC2 and demonstrates potent antitumor activity in experimental cancer models. | ||
| E2391 | α-Linolenic acid | α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties. | ||
| S8917 | P110δ-IN-1 | P110δ-IN-1 is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay. | ||
| E5889New | PI3K/Akt/mTOR-IN-2 | PI3K/Akt/mTOR-IN-2 is a specific inhibitor of the PI3K/Akt/mTOR signaling pathway. It exhibits an effective anti-cancer activity with IC50 value of 2.29 μM and can induce cancer cell cycle arrest and apoptosis. | ||
| S3575 | Zandelisib | Zandelisib(ME-401; PWT-143) is an orally bioavailable inhibitor of the phosphatidylinositide 3-kinase (PI3K). It selectively inhibits the delta isoform of PI3K (p110δ) and prevents the activation of the PI3K/AKT signaling pathway with an IC50 of 3.5 nM. It functions as an antineoplastic agent. | ||
| S7335 | IPI-3063 | IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. | ||
| E6051New | niclosamide ethanolamine | Niclosamide ethanolamine (Niclosamide-olamine, BAY2353 olamine) is a mild mitochondrial uncoupler, anthelmintic agent, and highly potent inhibitor of STAT3 signaling pathway with an IC50 of 0.25 μM. It improves insulin levels, body weight, and muscle wasting, inhibits artery constriction, suppresses PI3K-mTORC1 signaling to block fibroblast proliferation, inhibits TGF-β1-induced EMT and ECM accumulation via the mTORC1-4EBP1 axis, activates noncanonical autophagy to sensitize fibroblasts to apoptosis, and confers renoprotection in diabetic and adriamycin-induced nondiabetic kidney disease models. | ||
| E0121 | Parsaclisib (INCB050465) | Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. | ||
| E1579 | UCL-TRO-1938 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects. | ||
| E1834 | iMDK | iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC. | ||
| E2401 | SPP-86 | SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||
| E4680 | MTX-531 | MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers. | ||
| S5383 | Erucic acid | Erucic acid (cis-13-docosenoic acid) is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel. | ||
| E5872New | BBO-10203 | BBO - 10203は、PI3KαとKRASG12Cの強力な阻害剤であり、PI3KαのRAS結合ドメイン内のCys242に選択的かつ共有結合的に結合し、KRASG12CのGTP結合状態とGDP結合状態の両方を阻害し、IC50は0.031 nM、EC50は0.02 nMである。BBO - 10203は、RASアイソフォームとPI3Kαの相互作用を阻害し、RAS介在性のPI3Kα活性化を阻害し、pERKの発現を低下させ、細胞増殖を抑制し、G1期停止とアポトーシスを誘導する。BBO - 10203は、乳がん、結腸直腸がん、非小細胞肺がんの研究に使用できる。 | ||
| S1273 | Amarogentin | Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM. |
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| E4702 | SRX3177 | SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of 33 nM for BRD4 BD1, 89 nM for BRD4 BD2, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, <2.5 nM for CDK4, and 3.3 nM for CDK6. By simultaneously inhibiting these key pathways, SRX3177 disrupts cancer cell signalling and exhibits significant cytotoxic effects in tumors. | ||
| S3241 | Loureirin A | Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation. | ||
| S1105 | LY294002 | LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓ を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。 |
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| S2767 | 3-Methyladenine (3-MA) | 3-Methyladenine (3-MA)は、HeLa細胞におけるVps34およびPI3Kγに対する選択的PI3K阻害剤であり、IC50はそれぞれ25 μMと60 μMです。クラスI PI3Kを一貫して阻害する一方、クラスIII PI3Kの抑制は一時的であり、autophagosome形成も阻害します。溶液は不安定なため、使用直前に調製する必要があります。 |
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| S1009 | Dactolisib (BEZ235) | Dactolisib (BEZ235, NVP-BEZ235)は、ATP競合的なデュアルPI3KおよびmTOR阻害剤であり、p110α/γ/δ/βおよびmTOR(p70S6K)に対し、それぞれ細胞を含まないアッセイでIC50が4 nM /5 nM /7 nM /75 nM /6 nMです。3T3TopBP1-ER細胞においてATRをIC50 21 nMで阻害します。Dactolisibはautophagyを誘導し、HIV-1の複製を抑制します。フェーズ2。 |
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| S1065 | Pictilisib (GDC-0941) | Pictilisib (GDC-0941, RG7321) は、PI3Kα/δ の強力な阻害剤で、無細胞アッセイでは IC50 が 3 nM であり、p110β (11 倍) および p110γ (25 倍) に対しては控えめな選択性を示します。Pictilisib (GDC-0941) は autophagy および apoptosis を誘導します。フェーズ 2。 |
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| S2758 | Wortmannin (SL-2052) | Wortmanninは、初めて記述されたPI3K阻害剤で、細胞を含まないアッセイでのIC50は3 nMであり、PI3Kファミリー内での選択性はほとんどありません。Wortmanninは、autophagosomeの形成を阻害し、細胞を含まないアッセイでIC50が16 nMおよび150 nMでDNA-PK/ATMを強力に阻害します。Wortmanninはまた、PLK1活性も阻害します。 |
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| S2638 | NU7441 (KU-57788) | NU7441 (KU-57788) は、IC50が14 nMの非常に強力で選択的なDNA-PK阻害剤であり、セルリーアッセイにおいてmTORとPI3Kをそれぞれ1.7 μMと5 μMのIC50で阻害します。Cas9を介したDNA切断後、NHEJの頻度を減少させ、HDRの速度を増加させます。 |
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| S2226 | CAL-101 (Idelalisib) | Idelalisib (CAL-101)は、セルフリーアッセイにおいて2.5 nMのIC50を持つ選択的p110δ阻害剤であり、p110α/β/γよりも40〜300倍、C2β、hVPS34、DNA-PK、mTORよりも400〜4000倍高いp110δ選択性を示します。Idelalisibはまた、autophagyを刺激します。 |
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| S2247 | Buparlisib (BKM120) | Buparlisib (BKM120, NVP-BKM120) は、細胞を使用しないアッセイでそれぞれ 52 nM/166 nM/116 nM/262 nM の IC50 を持つ、p110α/β/δ/γ の選択的 PI3K 阻害剤です。VPS34、mTOR、DNAPK に対する効力は低下しており、PI4Kβ に対する活性はほとんどありません。Buparlisib はアポトーシスを誘導します。第2相。 |
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| S2814 | Alpelisib (BYL719) | アルペリシブ (Alpelisib (BYL719)) はPI3Kβ/γ/δ に対する影響が最小限の、強力かつ選択的な PI3Kα 阻害剤(無細胞アッセイで IC50 = 5 nM) です。 臨床フェーズ2。 |
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| S1038 | PI-103 | PI-103 は、無細胞アッセイにおいて IC50 が 2 nM/3 nM/3 nM/15 nM の p110α/β/δ/γ を標的とするマルチ PI3K 阻害剤で、mTOR/DNA-PK に対しては IC50 が 30 nM/23 nM と効力は低い。PI-103 はマウス T 細胞リンパ腫で apoptosis を誘導する。 |
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| S1169 | TGX-221 | TGX-221は、細胞を含まないアッセイで5 nMのIC50を持つp110β特異的阻害剤であり、p110αよりも1000倍p110βに対して選択的です。 |
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| S1072 | ZSTK474 | ZSTK474は、細胞を含まないアッセイで、主にPI3KδであるクラスI PI3Kアイソフォームを37 nMのIC50で阻害します。フェーズ1/2。 |
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| S2893 | NU7026 | NU7026 (LY293646) は、細胞フリーアッセイにおいてIC50が0.23 µMの強力なDNA-PK阻害剤であり、PI3Kに対しては60倍の選択性を示し、ATMおよびATRの両方に対しては不活性です。NU7026はG2/M細胞周期停止とアポトーシスを促進します。 |
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| S2658 | Omipalisib (GSK2126458) | Omipalisib (GSK2126458, GSK458) は、p110α/β/δ/γ および mTORC1/2 の高選択的かつ強力な阻害剤であり、セル-フリーアッセイにおけるKi値はそれぞれ0.019 nM/0.13 nM/0.024 nM/0.06 nM、および0.18 nM/0.3 nMです。Omipalisib はautophagyを誘導します。フェーズ1。 |
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| S2802 | Copanlisib (BAY 80-6946) | Copanlisibは、PI3Kα/β/γ/δのセル・フリーアッセイにおいて、それぞれ0.5、3.7、6.4、0.7 nMのIC50を持つ強力なパンクラスI PI3Kです。フェーズ3。本製品は溶解度が低く、動物実験には使用できますが、細胞実験には慎重にお選びください。 |
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| S2636 | A66 | A66は、無細胞アッセイにおいてIC50が32 nMである強力かつ特異的なp110α阻害剤であり、他のクラスI PI3Kアイソフォームと比較してp110αに対する100倍以上の選択性を示します。 |
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| S2391 | Quercetin (Sophoretin) | 野菜、果物、ワインに含まれる天然フラボノイドであるQuercetinは、組換えSIRT1の刺激剤であり、IC50が2.4-5.4 µMのPI3K阻害剤でもあります。Quercetinはmitophagy、apoptosis、および防御的autophagyを誘導します。フェーズ4。 |
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| S2743 | PF-04691502 | PF-04691502（PF4691502）は、ATP競合的なPI3K(α/β/δ/γ)/mTORデュアル阻害剤であり、セルフリーアッセイにおいてKi値が1.8 nM/2.1 nM/1.6 nM/1.9 nMおよび16 nMですが、Vps34、AKT、PDK1、p70S6K、MEK、ERK、p38、またはJNKに対してはほとんど活性がありません。PF-04691502はapoptosisを誘導します。フェーズ2。 |
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| S7028 | IPI-145 (Duvelisib) | Duvelisib (IPI-145, INK1197) は、新規かつ選択的なPI3K δ/γ阻害剤であり、セル-フリーアッセイにおけるKiおよびIC50は23 pM/243 pMおよび1 nM/50 nMで、他のプロテインキナーゼよりもPI3K δ/γに対して高い選択性を示します。フェーズ3。 |
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| S1205 | PIK-75 HCl | PIK-75 HClは、p110α阻害剤であり、IC50は5.8 nM（p110βよりも200倍強力）、Ser773のアイソフォーム特異的変異体を持ち、また無細胞アッセイではDNA-PKをIC50 2 nMで強力に阻害します。 |
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| S7682 | SAR405 | SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells. |
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| S1268 | IC-87114 | IC-87114は、無細胞アッセイにおいてIC50が0.5 µMの選択的PI3Kδ阻害剤であり、PI3Kγよりも58倍、PI3Kα/βよりも100倍以上選択性が高いです。 |
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| S2298 | Fisetin | Fisetin（フィセチン）は、強力なsirtuin活性化化合物（STAC）であり、sirtuinsを調節する薬剤です。 |
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| S1410 | AS-605240 | AS-605240は、細胞を含まないアッセイにおいて、PI3Kδ/βおよびPI3KαよりもPI3Kγに対してそれぞれ30倍および7.5倍以上選択的であり、PI3Kγを8 nMのIC50で選択的に阻害します。 |
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| S7103 | Taselisib (GDC 0032) | Taselisib (GDC 0032, RG7604)は、強力な次世代βアイソフォーム温存PI3K阻害剤であり、PI3Kα/δ/γを標的とし、Ki値は0.29 nM/0.12 nM/0.97 nMで、PI3Kβに対して10倍以上の選択性を示します。 | ||
| S1362 | Rigosertib (ON-01910) | Rigosertib (ON-01910) は、無細胞アッセイにおいてIC50が9 nMの非ATP競争的PLK1阻害剤です。Plk2に対して30倍高い選択性を示し、Plk3には活性がありません。RigosertibはPI3K/Akt経路を阻害し、酸化的ストレスシグナルを活性化します。Rigosertibは様々な癌細胞でapoptosisを誘導します。現在フェーズ3です。 |
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| S2759 | Fimepinostat (CUDC-907) | CUDC-907は、PI3KαとHDAC1/2/3/10に対するデュアルPI3KおよびHDAC阻害剤であり、それぞれ19 nMと1.7 nM/5 nM/1.8 nM/2.8 nMのIC50を示します。CUDC-907は、乳がん細胞において細胞周期停止とapoptosisを誘導します。第1相。 |
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| S7980 | VPS34-IN1 | Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy. |
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| S2696 | Apitolisib (GDC-0980) | Apitolisib (GDC-0980, RG7422, GNE 390) は、クラスI PI3K の強力な阻害剤であり、セルリーアッセイにおいてPI3Kα/β/δ/γ に対するIC50 はそれぞれ5 nM/27 nM/7 nM/14 nM です。また、mTOR 阻害剤でもあり、セルリーアッセイにおけるKi は17 nM で、他のPIKKファミリーキナーゼに対して高い選択性を示します。Apitolisib は、膵臓癌細胞においてAutophagy とApoptosis を同時に活性化します。現在、第2相臨床試験中です。 |
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| S1187 | PIK-90 | PIK-90は、PI3Kα/γ/δ阻害剤であり、それぞれ11 nM/18 nM/58 nMのIC50を持ち、PI3Kβには効力が劣ります。 |
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| S2628 | Gedatolisib (PKI-587) | Gedatolisib (PF-05212384, PKI-587) は、PI3Kα、PI3Kγ、mTORの強力なデュアル阻害剤であり、それぞれセルアッセイでIC50が0.4 nM、5.4 nM、1.6 nMでした。フェーズ2。 |
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| S8330 | Eganelisib (IPI-549) | Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM. | ||
| S1462 | AZD6482 | AZD6482 (KIN-193)は、PI3Kβ阻害剤であり、細胞を含まないアッセイにおいて、PI3Kδ、PI3Kα、およびPI3KγよりもPI3Kβに対して8倍、87倍、109倍選択的であり、IC50は10 nMです。フェーズ1。 |
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| S7683 | PIK-III | PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
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| S7356 | HS-173 | HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. |
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| S2671 | AS-252424 | AS-252424は、新規かつ強力なPI3Kγ阻害剤であり、セルフリーアッセイにおいてIC50は30 nMであり、PI3Kαと比較してPI3Kγに対する選択性は30倍高く、PI3Kδ/βに対する阻害活性は低い。 |
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| S7694 | AZD8186 | AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1. | ||
| S8002 | GSK2636771 | GSK2636771は、PI3Kα/PI3Kγに対して900倍以上、PI3Kδに対して10倍以上の選択性を持つ、強力で経口投与可能かつ選択的なPI3Kβ阻害剤です。PTEN欠損細胞株に感受性を示します。 |
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| S1219 | YM201636 | YM201636は、33 nMのIC50を持つ選択的なPIKfyve阻害剤であり、p110αには効力が低く、Fabl（酵母オーソログ）には不感応です。YM-201636は、autophagyの誘導を介して肝臓がんの増殖を抑制します。 |
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| S7016 | VS-5584 (SB2343) | VS-5584 (SB2343)は、強力で選択的なデュアルPI3K/mTOR阻害剤で、mTOR、PI3Kα/β/δ/γに対してそれぞれIC50値が3.4 nMおよび2.6-21 nMです。第1相。 |
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| S7645 | Pilaralisib (XL147) | Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2. |
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| S1360 | GSK1059615 | GSK1059615は、PI3Kα/β/δ/γ（可逆的）およびmTORのデュアル阻害剤であり、それぞれ0.4 nM/0.6 nM/2 nM/5 nMおよび12 nMのIC50を示します。フェーズ1。 |
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| S7018 | CZC24832 | CZC24832は、PI3Kγを27 nMのIC50で阻害する初の選択的阻害剤であり、PI3Kβに対して10倍、PI3KαおよびPI3Kδに対して100倍以上の選択性を示します。 |
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| S1352 | TG100-115 | TG100-115は、PI3Kγ/δ阻害剤であり、IC50は83 nM/235 nMで、PI3Kα/βにはほとんど影響を与えません。フェーズ1/2。 |
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| S7646 | Voxtalisib (XL765) | Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
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| S2749 | BGT226 (NVP-BGT226) maleate | BGT226 (NVP-BGT226)は、IC50が4 nM/63 nM/38 nMのPI3Kα/β/γに対する新規クラスI PI3K/mTOR阻害剤です。臨床第1/2相。 |
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| S8322 | Samotolisib (LY3023414) | LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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| S1118 | XL147 analogue | XL147 analogue (SAR245408)は、細胞を含まないアッセイにおいてIC50が39 nM/36 nM/23 nMのPI3Kα/δ/γに対する選択的かつ可逆的なクラスI PI3K inhibitorであり、PI3Kβに対しては効力が劣ります。XL147 analogueはapoptosisを誘導します。第1/2相。 |
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| S2681 | AS-604850 | AS-604850は、選択的ATP競合的PI3Kγ阻害剤であり、IC50は250 nMです。PI3Kδ/βに対するPI3Kγの選択性は80倍以上であり、PI3Kαに対するPI3Kγの選択性は18倍です。 |
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| S8045 | KU-0060648 | KU-0060648は、DNA-PKおよびPI3Kα、PI3Kβ、PI3Kδのデュアル阻害剤であり、それぞれのIC50は8.6 nM、4 nM、0.5 nM、0.1 nMです。PI3Kγに対する阻害は少なく、IC50は0.59 μMです。 |
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| S8674 | GO-203 TFA | GO-203 is a D-amino acid cell-penetrating peptide inhibitor of MUC1-C dimerization and thereby its oncogenic function. | ||
| S8596 | Autophinib | Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro. | ||
| S2347 | Quercetin Dihydrate | リンゴ、タマネギ、ベリー、赤ワインなど、さまざまな植物性食品に含まれるポリフェノール性フラボノイドであるQuercetin (Sophoretin)は、神経系および抗がん効果のために多くの異なる文化で利用されています。天然のフラボノイドであるQuercetin (dihydrate)は、組換えSIRT1の刺激剤であり、PI3K γ、PI3K δ、PI3K βに対してそれぞれ2.4 μM、3.0 μM、5.4 μMのIC50値を持つPI3K阻害剤です。 |
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| S8456 | VPS34 inhibitor 1 (Compound 19) | VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM. |
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| S8194 | umbralisib (TGR-1202) | Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. | ||
| S1523 | Voxtalisib (XL765) Analogue | Voxtalisib (SAR245409, XL765) Analogue は、mTOR/PI3K のデュアルインヒビターであり、主に p110γ に対して IC50 9 nM です。DNA-PK および mTOR も阻害します。第 1/2 相。 |
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| S2739 | PKI-402 | PKI-402は、PI3Kα/β/γ/δおよびmTORをそれぞれ2 nM/7 nM/16 nM/14 nMおよび3 nMのIC50で標的とする強力なデュアルpan-PI3K/mTOR阻害剤です。PI3Kα変異体E545KおよびH1047Rにも強力です。 | ||
| S8668 | GDC-0077 (Inavolisib) | Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3. | ||
| S7813 | AMG319 | AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. | ||
| S8738 | Bimiralisib (PQR309) | Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets. | ||
| S7937 | Nemiralisib | Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). | ||
| S8132 | Deguelin | Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor. | ||
| S2699 | CH5132799 | CH5132799（MEN1611、PA799）は、クラスIのPI3Ksを阻害し、特にPI3KαをIC50 14 nMで阻害します。PI3Kβδγに対しては効果が低いですが、PIK3CA変異細胞株には感受性を示します。第1相。 |
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| S8163 | Paxalisib (GDC-0084) | Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR. | ||
| S8581 | Serabelisib (TAK-117) | Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. | ||
| S2227 | PIK-294 | PIK-294は、p110δに対する高選択的阻害剤であり、IC50は10 nMで、それぞれPI3Kα/β/γに対して1000倍、49倍、16倍効力が低い。 |
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| S2870 | TG100713 | TG100713は、PI3Kγ、PI3Kδ、PI3Kα、PI3Kβに対するパンPI3K阻害剤であり、それぞれのIC50は50 nM、24 nM、165 nM、215 nMです。 |
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| S9190 | Oroxin B | Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment. | ||
| S3238 | Resibufogenin | Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. | ||
| S8589 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. | ||
| S7798 | GNE-317 | GNE-317 is a potent, brain-penetrant PI3K inhibitor. | ||
| S7966 | AZD8835 | AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). | ||
| S3220 | Trigonelline | Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells. | ||
| S6541 | MTX-211 | MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase. | ||
| S8157 | GDC-0326 | GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. | ||
| E2384 | (E)-Akt inhibitor-IV | (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic. | ||
| S3785 | Notoginsenoside R1 | Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways. | ||
| S7623 | PI-3065 | PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members. | ||
| S8693 | Selective PI3Kδ Inhibitor 1 (compound 7n) | Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. | ||
| S2682 | CAY10505 | CAY10505は、AS-252424の脱ヒドロキシ体であり、PI3Kγ阻害剤であり、IC50は33 nMです。 |
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| S3296 | Hispidulin | Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. | ||
| E8308New | Alpelisib hydrochloride | Alpelisib hydrochloride is a potent and selective inhibitor of PI3Kα with an IC50 of 0.005 μM, 1.2 μM, 0.29 μM, 0.25 μM for p110α, p110β, p110δ, p110γ, respectively. It exhibits good efficacy in inhibiting the growth of PI3Ka driven tumors and can be used in cancer research. | ||
| S0817 | SKI-V | SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity. | ||
| S8560 | Seletalisib (UCB-5857) | Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). | ||
| S8752 | leniolisib (CDZ 173) | Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. | ||
| S5978 | Gallein | Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain. | ||
| S5818 | acalisib (GS-9820) | Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. | ||
| S7675 | PF-4989216 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. | ||
| S6516 | GNE-477 | GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. | ||
| S6517 | GNE-493 | GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. | ||
| S2207 | PIK-293 | PIK-293はPI3K阻害剤であり、主にPI3Kδに対してIC50が0.24 μMで、PI3Kα/β/γに対してそれぞれ500倍、100倍、50倍効果が低い。 |
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| E5875New | LY294002 hydrochloride | LY294002 hydrochloride is a potent and specific inhibitor of PI3K with an IC50 of 0.5 μM, 0.97 μM, and 0.57 μM for P110α, P110β, P110δ, respectively. It also acts as a direct blocker of L-type Ca2+ channel with IC50 of 20 µM. | ||
| E1076New | Linperlisib | リンペルリシブは、特許WO 2015055071 A1の化合物10から抽出された強力で経口投与可能な選択的PI3Kδ阻害剤であり、IC50は6.4 nMである。 | ||
| E4683 | PI3K/AKT-IN-1 | PI3K/AKT-IN-1 is a dual-acting inhibitor of PI3K/AKT pathway with an IC50 of 6.99 µM, 4.01 µM, and 3.36 µM, for PI3Kδ, PI3Kγ and AKT-1 respectively. It also induces S-phase cell cycle arrest, caspase-3-dependent apoptosis, exhibiting strong potential against breast cancer and leukemia. | ||
| S3224 | Cinobufagin | Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. | ||
| S7938 | GSK2292767 | GSK2292767 is a potent and selective PI3Kδ inhibitor. | ||
| S5554 | Lanatoside C | Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways. | ||
| E2375 | PI3K/mTOR Inhibitor-2 | PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity. | ||
| S3243 | Zeaxanthin | Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM. | ||
| S0947 | Cafestol | Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60. | ||
| E4605New | Copanlisib dihydrochloride | Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a selective and potent inhibitor of pan-class I PI3K. It significantly inhibits the catalytic activity of class I PI3K isoforms α, β, γ, and δ with IC50 of 0.5, 3.7, 6.4, and 0.7 nM, respectively. BAY 80-6946 exhibits potent antitumor activity in multiple cell-line–derived and patient-derived xenograft tumor models. | ||
| E1609New | NVP-CLR457 | NVP-CLR457 is an orally active, potent, and balanced inhibitor of pan-class I PI3K. NVP-CLR457 exhibits IC50 values of 12 ± 1.5 nM, 8.3 ± 1.0 nM, 8.3 ± 2.0 nM, 230 ± 31 nM, for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ. It shows a clear dose-dependent PK/PD/efficacy relationship and demonstrates antitumor activity. | ||
| E4864 | Pentamidine | Pentamidine (MP-601205) is an aromatic diamidine drug, an antagonist of TLR4.It also inhibits PI3K/AKT signaling pathway and reduce the expression of MMP-2 and MMP-9. It exhibits anti- protozoal, anti-inflammatory, and anti-tumor activities and is used as an agent for treating African trypanosomiasis, antimony resistant leishmaniasis and Pneumocystis carinii pneumonia. | ||
| E2823 | PIK-108 | PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor. | ||
| E0020 | Lupenone | Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway. | ||
| E4765New | TYM-3-98 | TYM-3-98 is a selective inhibitor of PI3Kδ with an IC50 of 7.1 nM. It blocks the PI3Kδ/AKT signaling pathway, induces apoptosis in B-cell lymphomas, and effectively suppresses xenograft tumor growth in vivo. | ||
| E1815 | Tersolisib (STX-478) | Tersolisib (STX-478) is a highly potent, mutant-selective, allosteric inhibitor of PI3Kα, that selectively targets prevalent mutant forms of PI3Kα. It demonstrates strong efficacy against common PI3Kα helical- and kinase-domain mutations, including the H1047R variant, with an IC50 value of 9.4 nmol/L. STX-478 exhibits 14-fold greater selectivity for mutant PI3Kα over the wild-type form. It spares metabolic dysfunction and improves therapeutic response in PI3Kα-Mutant Xenografts. | ||
| E2366 | IHMT-PI3Kδ-372 | IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay | ||
| S8672 | Tenalisib | Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. | ||
| S3309 | Solasodine | Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21. | ||
| S9054 | Pectolinarin | Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway. | ||
| S8948 | SRX3207 | SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. | ||
| E5809 | Dactolisib Tosylate | Dactolisib Tosylate (BEZ235 Tosylate, NVP-BEZ 235 Tosylate) is an imidazo[4,5-c]quinoline derivative and dual inhibitor of PI3K/mTOR with IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. It blocks mTORC1/mTORC2 and demonstrates potent antitumor activity in experimental cancer models. | ||
| S8917 | P110δ-IN-1 | P110δ-IN-1 is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay. | ||
| E5889New | PI3K/Akt/mTOR-IN-2 | PI3K/Akt/mTOR-IN-2 is a specific inhibitor of the PI3K/Akt/mTOR signaling pathway. It exhibits an effective anti-cancer activity with IC50 value of 2.29 μM and can induce cancer cell cycle arrest and apoptosis. | ||
| S3575 | Zandelisib | Zandelisib(ME-401; PWT-143) is an orally bioavailable inhibitor of the phosphatidylinositide 3-kinase (PI3K). It selectively inhibits the delta isoform of PI3K (p110δ) and prevents the activation of the PI3K/AKT signaling pathway with an IC50 of 3.5 nM. It functions as an antineoplastic agent. | ||
| S7335 | IPI-3063 | IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. | ||
| E6051New | niclosamide ethanolamine | Niclosamide ethanolamine (Niclosamide-olamine, BAY2353 olamine) is a mild mitochondrial uncoupler, anthelmintic agent, and highly potent inhibitor of STAT3 signaling pathway with an IC50 of 0.25 μM. It improves insulin levels, body weight, and muscle wasting, inhibits artery constriction, suppresses PI3K-mTORC1 signaling to block fibroblast proliferation, inhibits TGF-β1-induced EMT and ECM accumulation via the mTORC1-4EBP1 axis, activates noncanonical autophagy to sensitize fibroblasts to apoptosis, and confers renoprotection in diabetic and adriamycin-induced nondiabetic kidney disease models. | ||
| E0121 | Parsaclisib (INCB050465) | Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. | ||
| E1834 | iMDK | iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC. | ||
| E2401 | SPP-86 | SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells. | ||
| E4680 | MTX-531 | MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers. | ||
| E5872New | BBO-10203 | BBO - 10203は、PI3KαとKRASG12Cの強力な阻害剤であり、PI3KαのRAS結合ドメイン内のCys242に選択的かつ共有結合的に結合し、KRASG12CのGTP結合状態とGDP結合状態の両方を阻害し、IC50は0.031 nM、EC50は0.02 nMである。BBO - 10203は、RASアイソフォームとPI3Kαの相互作用を阻害し、RAS介在性のPI3Kα活性化を阻害し、pERKの発現を低下させ、細胞増殖を抑制し、G1期停止とアポトーシスを誘導する。BBO - 10203は、乳がん、結腸直腸がん、非小細胞肺がんの研究に使用できる。 | ||
| S1273 | Amarogentin | Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM. |
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| E4702 | SRX3177 | SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of 33 nM for BRD4 BD1, 89 nM for BRD4 BD2, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, <2.5 nM for CDK4, and 3.3 nM for CDK6. By simultaneously inhibiting these key pathways, SRX3177 disrupts cancer cell signalling and exhibits significant cytotoxic effects in tumors. | ||
| S3241 | Loureirin A | Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation. | ||
| S7865 | 740 Y-P (PDGFR 740Y-P) | 740 Y-P (PDGFR 740Y-P, 740YPDGFR) is a cell-permeable phosphopeptide activator of PI3K. | ||
| E0785 | YS-49 | YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors. | ||
| S3294 | Demethyl-Coclaurine | Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes. | ||
| E2947 | Recilisib | Recilisib (ON01210, EX-RAD) is a radioprotectant that activates the activity of AKT and PI3K in cells. It has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. | ||
| E1579 | UCL-TRO-1938 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects. | ||
| S5383 | Erucic acid | Erucic acid (cis-13-docosenoic acid) is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel. | ||
| S6885 | Ailanthone | Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively. | ||
| S4572 | Homosalate | Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways. | ||
| E2391 | α-Linolenic acid | α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties. | ||
| E8308New | Alpelisib hydrochloride | Alpelisib hydrochloride is a potent and selective inhibitor of PI3Kα with an IC50 of 0.005 μM, 1.2 μM, 0.29 μM, 0.25 μM for p110α, p110β, p110δ, p110γ, respectively. It exhibits good efficacy in inhibiting the growth of PI3Ka driven tumors and can be used in cancer research. | ||
| E5875New | LY294002 hydrochloride | LY294002 hydrochloride is a potent and specific inhibitor of PI3K with an IC50 of 0.5 μM, 0.97 μM, and 0.57 μM for P110α, P110β, P110δ, respectively. It also acts as a direct blocker of L-type Ca2+ channel with IC50 of 20 µM. | ||
| E1076New | Linperlisib | リンペルリシブは、特許WO 2015055071 A1の化合物10から抽出された強力で経口投与可能な選択的PI3Kδ阻害剤であり、IC50は6.4 nMである。 | ||
| E4605New | Copanlisib dihydrochloride | Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a selective and potent inhibitor of pan-class I PI3K. It significantly inhibits the catalytic activity of class I PI3K isoforms α, β, γ, and δ with IC50 of 0.5, 3.7, 6.4, and 0.7 nM, respectively. BAY 80-6946 exhibits potent antitumor activity in multiple cell-line–derived and patient-derived xenograft tumor models. | ||
| E1609New | NVP-CLR457 | NVP-CLR457 is an orally active, potent, and balanced inhibitor of pan-class I PI3K. NVP-CLR457 exhibits IC50 values of 12 ± 1.5 nM, 8.3 ± 1.0 nM, 8.3 ± 2.0 nM, 230 ± 31 nM, for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ. It shows a clear dose-dependent PK/PD/efficacy relationship and demonstrates antitumor activity. | ||
| E4765New | TYM-3-98 | TYM-3-98 is a selective inhibitor of PI3Kδ with an IC50 of 7.1 nM. It blocks the PI3Kδ/AKT signaling pathway, induces apoptosis in B-cell lymphomas, and effectively suppresses xenograft tumor growth in vivo. | ||
| E5889New | PI3K/Akt/mTOR-IN-2 | PI3K/Akt/mTOR-IN-2 is a specific inhibitor of the PI3K/Akt/mTOR signaling pathway. It exhibits an effective anti-cancer activity with IC50 value of 2.29 μM and can induce cancer cell cycle arrest and apoptosis. | ||
| E6051New | niclosamide ethanolamine | Niclosamide ethanolamine (Niclosamide-olamine, BAY2353 olamine) is a mild mitochondrial uncoupler, anthelmintic agent, and highly potent inhibitor of STAT3 signaling pathway with an IC50 of 0.25 μM. It improves insulin levels, body weight, and muscle wasting, inhibits artery constriction, suppresses PI3K-mTORC1 signaling to block fibroblast proliferation, inhibits TGF-β1-induced EMT and ECM accumulation via the mTORC1-4EBP1 axis, activates noncanonical autophagy to sensitize fibroblasts to apoptosis, and confers renoprotection in diabetic and adriamycin-induced nondiabetic kidney disease models. | ||
| E5872New | BBO-10203 | BBO - 10203は、PI3KαとKRASG12Cの強力な阻害剤であり、PI3KαのRAS結合ドメイン内のCys242に選択的かつ共有結合的に結合し、KRASG12CのGTP結合状態とGDP結合状態の両方を阻害し、IC50は0.031 nM、EC50は0.02 nMである。BBO - 10203は、RASアイソフォームとPI3Kαの相互作用を阻害し、RAS介在性のPI3Kα活性化を阻害し、pERKの発現を低下させ、細胞増殖を抑制し、G1期停止とアポトーシスを誘導する。BBO - 10203は、乳がん、結腸直腸がん、非小細胞肺がんの研究に使用できる。 |
PI3Kシグナル伝達経路
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間