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HDAC
HDAC製品
- All (90)
- HDAC阻害剤 (88)
- HDAC活性剤(1)
- HDACモジュレータ(1)
- 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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| S1047 | Vorinostat (SAHA) | Vorinostat (SAHA)は、細胞フリーアッセイにおいてIC50が~10 nMのHDAC阻害剤です。Vorinostatは、生産的なHPV-18 DNA増幅を無効にします。 |
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| S1053 | Entinostat (MS-275) | Entinostat (MS-275, SNDX-275) は、無細胞アッセイにおいてIC50が0.51 μMおよび1.7 μMでHDAC1およびHDAC3を強力に阻害し、HDACs 4、6、8、10と比較して優れています。Entinostatはautophagyとapoptosisを誘導します。フェーズ3。 |
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| S1030 | Panobinostat (LBH589) | Panobinostat (LBH589, NVP-LBH589) は、新しい広範囲スペクトルのHDAC阻害剤であり、in vitroアッセイでのIC50は5 nMです。Panobinostat (LBH589) はautophagyとapoptosisを誘発します。Panobinostat はin vivoでHIVの潜伏を効果的に阻害します。現在フェーズ3です。 |
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| S1045 | Trichostatin A (TSA) | トリコスタチンA (TSA (Trichostatin A) ) は HDAC 阻害剤であり、IC50 は cell-free assay において < 1.8 nM です。 |
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| S3020 | Romidepsin (FK228) | ロミデプシン (Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)) は強力な HDAC1 および HDAC2 阻害剤 (無細胞アッセイで IC50 = 36 nM/47 nM) です。 ロミデプシン (FK228/Depsipeptide) は、神経芽腫腫瘍細胞 (neuroblastoma tumor cells) の増殖を制御し、アポトーシス (apoptosis) を誘導します。 |
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| S1122 | Mocetinostat (MGCD0103) | Mocetinostat (MGCD0103, MG0103) は、強力なHDAC阻害剤であり、セルフリーアッセイにおいてHDAC1に対し0.15 μMのIC50を示し、HDAC2、3、11に対して2～10倍の選択性があり、HDAC4、5、6、7、8に対しては活性がありません。Mocetinostat (MGCD0103) はapoptosisとautophagyを誘導します。現在、第2相臨床試験中です。 |
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| S7229 | RGFP966 | RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC. |
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| S8049 | Tubastatin A | Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
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| S1085 | Belinostat (PXD101) | Belinostatは、細胞フリーアッセイで27 nMのIC50を持つ新規のHDAC阻害剤であり、シスプラチン耐性腫瘍で活性が実証されています。Belinostat（PXD101）はautophagyを誘導します。 |
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| S1396 | Resveratrol (trans-Resveratrol) | Resveratrolは、シクロオキシゲナーゼ（例：COX、IC50=1.1 μM）、リポキシゲナーゼ（LOX、IC50=2.7 μM）、キナーゼ、Sirtuin、その他のタンパク質を含む幅広い標的を持っています。抗がん作用、抗炎症作用、血糖降下作用、その他心血管に良い効果があります。Resveratrolはmitophagy/autophagyおよびオートファジー依存性apoptosisを誘導します。 |
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| S8001 | Ricolinostat (ACY-1215) | Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2. |
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| S1096 | Quisinostat (JNJ-26481585) Dihydrochloride | Quisinostat (JNJ-26481585) 2HClは、新規の第2世代HDAC阻害剤で、無細胞アッセイにおいてHDAC1に対するIC50が0.11 nMと最も高い効力を示し、HDACs 2、4、10、および11に対しては中程度の効力があります。HDACs 3、5、8、および9に対しては30倍以上の選択性を示し、HDACs 6および7に対しては最も低い効力です。フェーズ2。 |
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| S2012 | PCI-34051 | PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis. |
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| S1484 | MC1568 | MC1568は、無細胞アッセイにおいて100 nMのIC50を持つトウモロコシHD1-Aの選択的HDAC阻害剤です。HD1-BよりもHD1-Aに対して34倍選択的です。 |
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| S1848 | Curcumin | Curcumin (Diferuloylmethane, Natural Yellow 3, ウコン色素) は、ショウガ科 (Zingiberaceae) に属する人気のインドスパイスであるウコンの主要なクルクミノイドです。p300 histone acetylatransferase (IC50~25 μM) および Histone deacetylase (HDAC) の阻害剤であり、Nrf2 pathway を活性化し、NF-κB の活性化を抑制します。Curcumin は抗腫瘍活性を伴うマイトファジー、autophagy、apoptosis、および細胞周期停止を誘導します。Curcumin は、Ferroptosis を介した細胞死を減少させることにより、横紋筋融解症に関連する腎臓損傷を軽減します。Curcumin は、influenza virus、hepatitis C virus、HIV など、さまざまなヒト病原体に対して抗感染特性を示します。 |
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| S2627 | Tubastatin A HCl | Tubastatin A HCl は、細胞を含まないアッセイで 15 nM の IC50 を持つ強力かつ選択的な HDAC6 阻害剤です。HDAC8 (57 倍以上) を除く他のすべてのアイソザイムに対して選択的です (1000 倍以上)。 |
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| S2818 | Tacedinaline (CI994) | Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3. |
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| S3944 | VPA (Valproic acid) | VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling. | ||
| S7569 | LMK-235 | LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively. |
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| S2759 | Fimepinostat (CUDC-907) | CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
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| S2239 | Tubacin | Tubacinは、in vitroアッセイでIC50が4 nMの、非常に強力で選択的な可逆性細胞透過性HDAC6阻害剤であり、HDAC1に対して約350倍の選択性を示します。Tubacinは、ウイルスRNA合成の減少を介して、日本脳炎ウイルスの複製を減少させます。 |
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| S1168 | Valproic Acid sodium | Valproic Acid sodiumは、HDAC2のプロテアソーム分解を選択的に誘導することによりHDAC阻害剤として作用し、てんかん、双極性障害の治療、および片頭痛の予防に使用されます。Valproic acidは、小細胞肺がん（SCLC）細胞においてNotch1シグナル伝達を誘導します。Valproic acidは、HIVおよび様々な癌の治療薬として研究が進められています。Valproic acid（VPA）は、BNIP3を上方制御することによりautophagyとmitophagyを誘導し、PGC-1αを上方制御することによりミトコンドリア生合成を誘導します。 |
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| S1999 | Sodium butyrate | Sodium butyrate (NaB、酪酸ナトリウム塩) は酪酸のナトリウム塩であり、histone deacetylase阻害剤であり、クラスIおよびIIのhistone deacetylase (HDACs) の亜鉛結合部位に競合的に結合します。Sodium butyrate (NaB) は、細胞周期の進行を阻害し、分化を促進し、いくつかの種類の癌細胞においてapoptosisおよびautophagyを誘導します。 |
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| S2170 | ITF-2357 (Givinostat) Hydrochloride Monohydrate | Givinostat (ITF2357) は、細胞を含まないアッセイで、トウモロコシのHD2、HD1B、およびHD1Aに対する強力なHDAC阻害剤であり、IC50はそれぞれ10 nM、7.5 nM、16 nMです。第2相。 |
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| S8567 | Tucidinostat (Chidamide) | Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. | ||
| S2244 | AR-42 | AR-42（HDAC-42）は、HDAC阻害剤であり、IC50は30 nMです。フェーズ1。 |
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| S7324 | TMP269 | TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
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| S2341 | (-)-Parthenolide | Nuclear Factor-κB経路の阻害剤である(-)-Parthenolideは、他のクラスI/II HDACsに影響を与えることなく、HDAC1タンパク質を特異的に枯渇させます。また、MDM2のユビキチン化を促進し、p53細胞機能を活性化します。 |
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| S7595 | Santacruzamate A (CAY10683) | Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs. |
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| S7596 | CAY10603 | CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs. |
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| S1515 | Pracinostat (SB939) | Pracinostat (SB939) は、HDAC6 を除く IC50 が 40-140 nM の強力な pan-HDAC 阻害剤です。クラス III アイソザイム SIRT I に対しては活性がありません。Pracinostat (SB939) は腫瘍細胞のアポトーシスを誘発します。フェーズ 2。 |
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| S3592 | 4-PBA (4-Phenylbutyric acid) | 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models. | ||
| S1090 | Abexinostat (PCI-24781) | Abexinostat (PCI-24781, CRA-024781) は、主にHDAC1 をターゲットとする新規の pan-HDAC 阻害剤で、Ki は 7 nM です。HDACs 2、3、6、および 10 に対して中程度の効力を持ち、HDAC8 に対しては 40 倍以上の選択性があります。第 1/2 相。 |
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| S7292 | RG2833 (RGFP109) | RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively. |
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| S1194 | CUDC-101 | CUDC-101は、HDAC、EGFR、HER2に対する強力な多標的阻害剤であり、IC50はそれぞれ4.4 nM、2.4 nM、15.7 nMです。クラスI/II HDACを阻害しますが、クラスIIIのSir-type HDACは阻害しません。フェーズ1。 |
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| S8502 | TMP195 | TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with Ki of 59, 60, 26 and 15nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. | ||
| S1095 | Dacinostat (LAQ824) | Dacinostat (LAQ824, NVP-LAQ824) は、IC50が32 nMの新規HDAC阻害剤であり、p21プロモーターを活性化することが知られています。 |
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| S5771 | Sulforaphane | Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis. | ||
| S4125 | 4-PBA (Sodium Phenylbutyrate) | 4-PBA (Sodium Phenylbutyrate) is a salt of 4-phenylbutyrate (4-PBA) or 4-phenylbutyric acid.Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders. |
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| S7617 | Tasquinimod | Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3. |
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| S1422 | Droxinostat | Droxinostat (NS 41080) は、HDAC、主にHDAC6および8の選択的阻害剤であり、IC50は2.47 μMおよび1.46 μMであり、HDAC3に対して8倍以上の選択性を示し、HDAC1、2、4、5、7、9、および10に対しては阻害作用を示しません。 |
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| S7473 | Nexturastat A | Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs. |
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| S8043 | Scriptaid | Scriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3. |
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| S7555 | Domatinostat (4SC-202) | Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. | ||
| S2779 | M344 (D 237) | M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation. |
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| S2693 | Resminostat | Resminostat (RAS2410) dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM. |
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| S8323 | ITSA-1 (ITSA1) | ITSA-1 (ITSA1) affects HDAC activity after TSA treatment but shows no activity towards other HDAC inhibitors. | ||
| S7689 | BG45 | BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. | ||
| S8464 | Citarinostat (ACY-241) | Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. | ||
| S6687 | SIS17 | SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. | ||
| S8495 | WT161 | WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis. | ||
| S8648 | ACY-738 | ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs. | ||
| S7278 | HPOB | HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs. |
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| S6738 | TC-H 106 | TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively. | ||
| S0709 | Tubastatin A TFA | Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. | ||
| S3981 | Sinapinic Acid | Sinapinic acid (Sinapic acid) is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) acts as an inhibitor of HDAC, with IC50 of 2.27 mM, and also inhibits ACE-I activity. | ||
| S5810 | UF010 | UF010 is a class I HDAC-selective inhibitor with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM and 15.3 nM for HDAC1, HDAC2, HDAC3, HDAC8, HDAC6 and HDAC10, respectively. | ||
| S0864 | ACY-775 | ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5 nM. | ||
| S8773 | TH34 | TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM). | ||
| E8178 | Quisinostat | Quisinostat(JNJ-26481585) is a potent and orally active second-generation inhibitor of pan-Histone Deacetylase (HDAC). It inhibits HDAC1, HDAC2, HDAC4, HDAC10, HDAC11 with IC50s of 0.11 nM , 0.33 nM , 0.64 nM , 0.46 nM, 0.37 nM respectively. It exhibits potent in vivo antitumor activity and potential clinical use in various solid and hematologic malignancies. | ||
| S1703 | Divalproex Sodium | Divalproex Sodiumは、腸溶性コーティングされた1：1のモル比でバルプロ酸ナトリウムとバルプロ酸の化合物を構成し、てんかんの治療に用いられるHDAC阻害剤です。 |
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| E0391 | BRD-6929 | BRD-6929 is an inhibitor of histone deacetylase 1 (HDAC1) and HDAC2 with an IC50s of 0.04 µM and 0.1 µM, respectively. It exhibits antiproliferative activities against a human cancer cell line (HCT116) and in human mammary epithelial cells (HMEC). | ||
| S1073 | BML-210 (CAY10433) | BML-210 (CAY10433) is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM. | ||
| S9262 | Raddeanin A | Raddeanin A (Raddeanin R3, NSC382873), a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity. | ||
| E6577New | 1-Naphthohydroxamic acid | 1-ナフトヒドロキサム酸（化合物2）は、IC50が14 μMの強力かつ選択的なHDAC8阻害剤です。1-ナフトヒドロキサム酸は、クラスIのHDAC1およびクラスIIのHDAC6（IC50 >100 μM）よりもHDAC8に対して選択性が高いです。1-ナフトヒドロキサム酸は、グローバルなヒストンH4のアセチル化を増加させず、また細胞内の総HDAC活性を低下させません。1-ナフトヒドロキサム酸はチューブリンのアセチル化を誘導することができます。 | ||
| E5952New | PT 3 | PT 3 is a benzamide-class, potent, and selective inhibitor of Histone Deacetylase 3 (HDAC3) with an IC50 of 245 nM. It crosses the blood-brain barrier and enhances learning and memory in novel object recognition models in mice. | ||
| E8292New | GEM144 | GEM144 is a potent and orally active dual inhibitor of DNA polymerase α (POLA1) and HDAC11 . It exhibits potent antiproliferative activity in vitro and antitumor efficacy in vivo by inducing p53 acetylation, p21 activation, G1/S cell cycle arrest, and apoptosis. | ||
| E1086 | KT-531 | KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms. | ||
| E1686 | SW-100 | SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. | ||
| E1580 | TNG260 | TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing. | ||
| E1469 | ITF3756 | ITF3756 is a selective histone deacetylase 6 (HDAC6) inhibitor bearing a pentaheterocyclic scaffold. It can be used in research of autoimmune disorders, neurodegenerative diseases, and cancer. | ||
| E1554 | Tefinostat(CHR-2845) | Tefinostat(CHR-2845) is a monocyte/macrophage-targeted inhibitor of pan-histone deacetylase (HDAC). Tefinostat undergoes cleavage mediated by the intracellular esterase human carboxylesterase-1 (hCE-1) to yield the active acid CHR-2847. In vitro studies reveal a specific heightened sensitivity of monocytoid leukemias to tefinostat. | ||
| S2190 | Pyroxamide (NSC 696085) | Pyroxamide(NSC 696085)は、アフィニティー精製されたHDAC1の強力な阻害剤であり、ID50は100 nMです。また、in vitroでヒト横紋筋肉腫の増殖抑制と細胞死を誘導します。 | ||
| S8743 | SKLB-23bb | SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. | ||
| S9275 | Isoguanosine | Isoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML.Isoguanosine is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium. | ||
| S6548 | NKL 22 | NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM. | ||
| S7726 | BRD73954 | BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively. | ||
| E0812 | CXD101 | CXD101 (HDAC-IN-4) is a potent, selective and orally active class I histone deacetylase (HDAC) inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. | ||
| E5948New | PB94 | PB94 is a potent and selective inhibitor of HDAC11 with an IC50 of 108 nM and exhibits >40-fold selectivity over other HDAC isoforms. It ameliorates neuropathic pain in mouse models and can be radiolabeled with carbon-11 as [¹¹C]PB94 for PET imaging, demonstrating significant brain uptake and potential for in vivo imaging applications. | ||
| S5905 | Suberohydroxamic acid | Suberohydroxamic acid (suberic bishydroxamic acid) is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively. | ||
| S8962 | BRD3308 | BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. | ||
| S7593 | Splitomicin | Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay. | ||
| E7940 | ACY-957 | ACY-957 is a selective chemical inhibitor of HDAC1 and HDAC2 with an IC50 values of 7 nM, 18 nM against HDAC1/2 respectively. It induces hemoglobin protein (HbF) in primary erythroid progenitor cells, including those from sickle cell patients, offering a promising approach for treating sickle cell disease (SCD) and β-thalassemia. | ||
| S5438 | Biphenyl-4-sulfonyl chloride | Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. | ||
| E5936New | FT895 | FT895は、IC50が3 nMの強力かつ選択的なHDAC11阻害剤です。 | ||
| S9934 | KA2507 | KA2507, a potent, orally active and selective HDAC6 inhibitor with IC50 of 2.5 nM, shows antitumor activities and immune modulatory effects in preclinical models. | ||
| S2132 | SR-4370 | SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. | ||
| E7481 | Givinostat | Givinostat is an orally active, hydroxamic acid-containing inhibitor of histone deacetylases (HDACs), with the potential to treat children with systemic juvenile idiopathic arthritis. It primarily targets Class I and II HDACs, with IC50 of 198 nM and 157 nM for HDAC1 and HDAC3, respectively. | ||
| S1313 | GSK3117391 | GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor. | ||
| S8769 | Tinostamustine(EDO-S101) | Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs). | ||
| S1047 | Vorinostat (SAHA) | Vorinostat (SAHA)は、細胞フリーアッセイにおいてIC50が~10 nMのHDAC阻害剤です。Vorinostatは、生産的なHPV-18 DNA増幅を無効にします。 |
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| S1053 | Entinostat (MS-275) | Entinostat (MS-275, SNDX-275) は、無細胞アッセイにおいてIC50が0.51 μMおよび1.7 μMでHDAC1およびHDAC3を強力に阻害し、HDACs 4、6、8、10と比較して優れています。Entinostatはautophagyとapoptosisを誘導します。フェーズ3。 |
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| S1030 | Panobinostat (LBH589) | Panobinostat (LBH589, NVP-LBH589) は、新しい広範囲スペクトルのHDAC阻害剤であり、in vitroアッセイでのIC50は5 nMです。Panobinostat (LBH589) はautophagyとapoptosisを誘発します。Panobinostat はin vivoでHIVの潜伏を効果的に阻害します。現在フェーズ3です。 |
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| S1045 | Trichostatin A (TSA) | トリコスタチンA (TSA (Trichostatin A) ) は HDAC 阻害剤であり、IC50 は cell-free assay において < 1.8 nM です。 |
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| S3020 | Romidepsin (FK228) | ロミデプシン (Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)) は強力な HDAC1 および HDAC2 阻害剤 (無細胞アッセイで IC50 = 36 nM/47 nM) です。 ロミデプシン (FK228/Depsipeptide) は、神経芽腫腫瘍細胞 (neuroblastoma tumor cells) の増殖を制御し、アポトーシス (apoptosis) を誘導します。 |
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| S1122 | Mocetinostat (MGCD0103) | Mocetinostat (MGCD0103, MG0103) は、強力なHDAC阻害剤であり、セルフリーアッセイにおいてHDAC1に対し0.15 μMのIC50を示し、HDAC2、3、11に対して2～10倍の選択性があり、HDAC4、5、6、7、8に対しては活性がありません。Mocetinostat (MGCD0103) はapoptosisとautophagyを誘導します。現在、第2相臨床試験中です。 |
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| S7229 | RGFP966 | RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC. |
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| S8049 | Tubastatin A | Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
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| S1085 | Belinostat (PXD101) | Belinostatは、細胞フリーアッセイで27 nMのIC50を持つ新規のHDAC阻害剤であり、シスプラチン耐性腫瘍で活性が実証されています。Belinostat（PXD101）はautophagyを誘導します。 |
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| S1396 | Resveratrol (trans-Resveratrol) | Resveratrolは、シクロオキシゲナーゼ（例：COX、IC50=1.1 μM）、リポキシゲナーゼ（LOX、IC50=2.7 μM）、キナーゼ、Sirtuin、その他のタンパク質を含む幅広い標的を持っています。抗がん作用、抗炎症作用、血糖降下作用、その他心血管に良い効果があります。Resveratrolはmitophagy/autophagyおよびオートファジー依存性apoptosisを誘導します。 |
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| S8001 | Ricolinostat (ACY-1215) | Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2. |
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| S1096 | Quisinostat (JNJ-26481585) Dihydrochloride | Quisinostat (JNJ-26481585) 2HClは、新規の第2世代HDAC阻害剤で、無細胞アッセイにおいてHDAC1に対するIC50が0.11 nMと最も高い効力を示し、HDACs 2、4、10、および11に対しては中程度の効力があります。HDACs 3、5、8、および9に対しては30倍以上の選択性を示し、HDACs 6および7に対しては最も低い効力です。フェーズ2。 |
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| S2012 | PCI-34051 | PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis. |
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| S1484 | MC1568 | MC1568は、無細胞アッセイにおいて100 nMのIC50を持つトウモロコシHD1-Aの選択的HDAC阻害剤です。HD1-BよりもHD1-Aに対して34倍選択的です。 |
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| S1848 | Curcumin | Curcumin (Diferuloylmethane, Natural Yellow 3, ウコン色素) は、ショウガ科 (Zingiberaceae) に属する人気のインドスパイスであるウコンの主要なクルクミノイドです。p300 histone acetylatransferase (IC50~25 μM) および Histone deacetylase (HDAC) の阻害剤であり、Nrf2 pathway を活性化し、NF-κB の活性化を抑制します。Curcumin は抗腫瘍活性を伴うマイトファジー、autophagy、apoptosis、および細胞周期停止を誘導します。Curcumin は、Ferroptosis を介した細胞死を減少させることにより、横紋筋融解症に関連する腎臓損傷を軽減します。Curcumin は、influenza virus、hepatitis C virus、HIV など、さまざまなヒト病原体に対して抗感染特性を示します。 |
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| S2627 | Tubastatin A HCl | Tubastatin A HCl は、細胞を含まないアッセイで 15 nM の IC50 を持つ強力かつ選択的な HDAC6 阻害剤です。HDAC8 (57 倍以上) を除く他のすべてのアイソザイムに対して選択的です (1000 倍以上)。 |
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| S2818 | Tacedinaline (CI994) | Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3. |
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| S3944 | VPA (Valproic acid) | VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling. | ||
| S7569 | LMK-235 | LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively. |
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| S2759 | Fimepinostat (CUDC-907) | CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
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| S2239 | Tubacin | Tubacinは、in vitroアッセイでIC50が4 nMの、非常に強力で選択的な可逆性細胞透過性HDAC6阻害剤であり、HDAC1に対して約350倍の選択性を示します。Tubacinは、ウイルスRNA合成の減少を介して、日本脳炎ウイルスの複製を減少させます。 |
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| S1168 | Valproic Acid sodium | Valproic Acid sodiumは、HDAC2のプロテアソーム分解を選択的に誘導することによりHDAC阻害剤として作用し、てんかん、双極性障害の治療、および片頭痛の予防に使用されます。Valproic acidは、小細胞肺がん（SCLC）細胞においてNotch1シグナル伝達を誘導します。Valproic acidは、HIVおよび様々な癌の治療薬として研究が進められています。Valproic acid（VPA）は、BNIP3を上方制御することによりautophagyとmitophagyを誘導し、PGC-1αを上方制御することによりミトコンドリア生合成を誘導します。 |
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| S1999 | Sodium butyrate | Sodium butyrate (NaB、酪酸ナトリウム塩) は酪酸のナトリウム塩であり、histone deacetylase阻害剤であり、クラスIおよびIIのhistone deacetylase (HDACs) の亜鉛結合部位に競合的に結合します。Sodium butyrate (NaB) は、細胞周期の進行を阻害し、分化を促進し、いくつかの種類の癌細胞においてapoptosisおよびautophagyを誘導します。 |
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| S2170 | ITF-2357 (Givinostat) Hydrochloride Monohydrate | Givinostat (ITF2357) は、細胞を含まないアッセイで、トウモロコシのHD2、HD1B、およびHD1Aに対する強力なHDAC阻害剤であり、IC50はそれぞれ10 nM、7.5 nM、16 nMです。第2相。 |
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| S8567 | Tucidinostat (Chidamide) | Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. | ||
| S2244 | AR-42 | AR-42（HDAC-42）は、HDAC阻害剤であり、IC50は30 nMです。フェーズ1。 |
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| S7324 | TMP269 | TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
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| S2341 | (-)-Parthenolide | Nuclear Factor-κB経路の阻害剤である(-)-Parthenolideは、他のクラスI/II HDACsに影響を与えることなく、HDAC1タンパク質を特異的に枯渇させます。また、MDM2のユビキチン化を促進し、p53細胞機能を活性化します。 |
-Parthenolide-S234101W0220161110.gif)
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| S7595 | Santacruzamate A (CAY10683) | Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs. |
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| S7596 | CAY10603 | CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs. |
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| S1515 | Pracinostat (SB939) | Pracinostat (SB939) は、HDAC6 を除く IC50 が 40-140 nM の強力な pan-HDAC 阻害剤です。クラス III アイソザイム SIRT I に対しては活性がありません。Pracinostat (SB939) は腫瘍細胞のアポトーシスを誘発します。フェーズ 2。 |
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| S3592 | 4-PBA (4-Phenylbutyric acid) | 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models. | ||
| S1090 | Abexinostat (PCI-24781) | Abexinostat (PCI-24781, CRA-024781) は、主にHDAC1 をターゲットとする新規の pan-HDAC 阻害剤で、Ki は 7 nM です。HDACs 2、3、6、および 10 に対して中程度の効力を持ち、HDAC8 に対しては 40 倍以上の選択性があります。第 1/2 相。 |
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| S7292 | RG2833 (RGFP109) | RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively. |
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| S1194 | CUDC-101 | CUDC-101は、HDAC、EGFR、HER2に対する強力な多標的阻害剤であり、IC50はそれぞれ4.4 nM、2.4 nM、15.7 nMです。クラスI/II HDACを阻害しますが、クラスIIIのSir-type HDACは阻害しません。フェーズ1。 |
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| S8502 | TMP195 | TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with Ki of 59, 60, 26 and 15nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. | ||
| S1095 | Dacinostat (LAQ824) | Dacinostat (LAQ824, NVP-LAQ824) は、IC50が32 nMの新規HDAC阻害剤であり、p21プロモーターを活性化することが知られています。 |
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| S5771 | Sulforaphane | Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis. | ||
| S4125 | 4-PBA (Sodium Phenylbutyrate) | 4-PBA (Sodium Phenylbutyrate) is a salt of 4-phenylbutyrate (4-PBA) or 4-phenylbutyric acid.Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders. |
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| S1422 | Droxinostat | Droxinostat (NS 41080) は、HDAC、主にHDAC6および8の選択的阻害剤であり、IC50は2.47 μMおよび1.46 μMであり、HDAC3に対して8倍以上の選択性を示し、HDAC1、2、4、5、7、9、および10に対しては阻害作用を示しません。 |
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| S7473 | Nexturastat A | Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs. |
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| S8043 | Scriptaid | Scriptaid (GCK 1026) is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3. |
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| S7555 | Domatinostat (4SC-202) | Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1. | ||
| S2779 | M344 (D 237) | M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation. |
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| S2693 | Resminostat | Resminostat (RAS2410) dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM. |
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| S7689 | BG45 | BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. | ||
| S8464 | Citarinostat (ACY-241) | Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3. | ||
| S6687 | SIS17 | SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. | ||
| S8495 | WT161 | WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis. | ||
| S8648 | ACY-738 | ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs. | ||
| S7278 | HPOB | HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs. |
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| S6738 | TC-H 106 | TC-H 106 (Pimelic Diphenylamide 106) is a slow, tight-binding inhibitor of class I histone deacetylases(HDAC) with Ki value of 148 nM, about 102 nM, 14 nM for HDAC1, HDAC2, HDAC3, respectively. | ||
| S0709 | Tubastatin A TFA | Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. | ||
| S3981 | Sinapinic Acid | Sinapinic acid (Sinapic acid) is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) acts as an inhibitor of HDAC, with IC50 of 2.27 mM, and also inhibits ACE-I activity. | ||
| S5810 | UF010 | UF010 is a class I HDAC-selective inhibitor with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM and 15.3 nM for HDAC1, HDAC2, HDAC3, HDAC8, HDAC6 and HDAC10, respectively. | ||
| S0864 | ACY-775 | ACY-775 is a potent and selective histone deacetylase 6 (HDAC6) inhibitor with IC50 of 7.5 nM. | ||
| S8773 | TH34 | TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM). | ||
| E8178 | Quisinostat | Quisinostat(JNJ-26481585) is a potent and orally active second-generation inhibitor of pan-Histone Deacetylase (HDAC). It inhibits HDAC1, HDAC2, HDAC4, HDAC10, HDAC11 with IC50s of 0.11 nM , 0.33 nM , 0.64 nM , 0.46 nM, 0.37 nM respectively. It exhibits potent in vivo antitumor activity and potential clinical use in various solid and hematologic malignancies. | ||
| S1703 | Divalproex Sodium | Divalproex Sodiumは、腸溶性コーティングされた1：1のモル比でバルプロ酸ナトリウムとバルプロ酸の化合物を構成し、てんかんの治療に用いられるHDAC阻害剤です。 |
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| E0391 | BRD-6929 | BRD-6929 is an inhibitor of histone deacetylase 1 (HDAC1) and HDAC2 with an IC50s of 0.04 µM and 0.1 µM, respectively. It exhibits antiproliferative activities against a human cancer cell line (HCT116) and in human mammary epithelial cells (HMEC). | ||
| S1073 | BML-210 (CAY10433) | BML-210 (CAY10433) is a small molecule inhibitor of HDAC.BML-210 inhibits the HDAC4-VP16-driven reporter signal in a dose-dependent manner with an apparent IC50 of ∼5 µM. | ||
| S9262 | Raddeanin A | Raddeanin A (Raddeanin R3, NSC382873), a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity. | ||
| E6577New | 1-Naphthohydroxamic acid | 1-ナフトヒドロキサム酸（化合物2）は、IC50が14 μMの強力かつ選択的なHDAC8阻害剤です。1-ナフトヒドロキサム酸は、クラスIのHDAC1およびクラスIIのHDAC6（IC50 >100 μM）よりもHDAC8に対して選択性が高いです。1-ナフトヒドロキサム酸は、グローバルなヒストンH4のアセチル化を増加させず、また細胞内の総HDAC活性を低下させません。1-ナフトヒドロキサム酸はチューブリンのアセチル化を誘導することができます。 | ||
| E5952New | PT 3 | PT 3 is a benzamide-class, potent, and selective inhibitor of Histone Deacetylase 3 (HDAC3) with an IC50 of 245 nM. It crosses the blood-brain barrier and enhances learning and memory in novel object recognition models in mice. | ||
| E8292New | GEM144 | GEM144 is a potent and orally active dual inhibitor of DNA polymerase α (POLA1) and HDAC11 . It exhibits potent antiproliferative activity in vitro and antitumor efficacy in vivo by inducing p53 acetylation, p21 activation, G1/S cell cycle arrest, and apoptosis. | ||
| E1086 | KT-531 | KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms. | ||
| E1686 | SW-100 | SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. | ||
| E1580 | TNG260 | TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing. | ||
| E1469 | ITF3756 | ITF3756 is a selective histone deacetylase 6 (HDAC6) inhibitor bearing a pentaheterocyclic scaffold. It can be used in research of autoimmune disorders, neurodegenerative diseases, and cancer. | ||
| E1554 | Tefinostat(CHR-2845) | Tefinostat(CHR-2845) is a monocyte/macrophage-targeted inhibitor of pan-histone deacetylase (HDAC). Tefinostat undergoes cleavage mediated by the intracellular esterase human carboxylesterase-1 (hCE-1) to yield the active acid CHR-2847. In vitro studies reveal a specific heightened sensitivity of monocytoid leukemias to tefinostat. | ||
| S2190 | Pyroxamide (NSC 696085) | Pyroxamide(NSC 696085)は、アフィニティー精製されたHDAC1の強力な阻害剤であり、ID50は100 nMです。また、in vitroでヒト横紋筋肉腫の増殖抑制と細胞死を誘導します。 | ||
| S8743 | SKLB-23bb | SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability. | ||
| S9275 | Isoguanosine | Isoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML.Isoguanosine is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium. | ||
| S6548 | NKL 22 | NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM. | ||
| S7726 | BRD73954 | BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively. | ||
| E0812 | CXD101 | CXD101 (HDAC-IN-4) is a potent, selective and orally active class I histone deacetylase (HDAC) inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. | ||
| E5948New | PB94 | PB94 is a potent and selective inhibitor of HDAC11 with an IC50 of 108 nM and exhibits >40-fold selectivity over other HDAC isoforms. It ameliorates neuropathic pain in mouse models and can be radiolabeled with carbon-11 as [¹¹C]PB94 for PET imaging, demonstrating significant brain uptake and potential for in vivo imaging applications. | ||
| S5905 | Suberohydroxamic acid | Suberohydroxamic acid (suberic bishydroxamic acid) is a competitive HDAC inhibitor with IC50 values of 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively. | ||
| S8962 | BRD3308 | BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release. | ||
| S7593 | Splitomicin | Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay. | ||
| E7940 | ACY-957 | ACY-957 is a selective chemical inhibitor of HDAC1 and HDAC2 with an IC50 values of 7 nM, 18 nM against HDAC1/2 respectively. It induces hemoglobin protein (HbF) in primary erythroid progenitor cells, including those from sickle cell patients, offering a promising approach for treating sickle cell disease (SCD) and β-thalassemia. | ||
| S5438 | Biphenyl-4-sulfonyl chloride | Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. | ||
| E5936New | FT895 | FT895は、IC50が3 nMの強力かつ選択的なHDAC11阻害剤です。 | ||
| S9934 | KA2507 | KA2507, a potent, orally active and selective HDAC6 inhibitor with IC50 of 2.5 nM, shows antitumor activities and immune modulatory effects in preclinical models. | ||
| S2132 | SR-4370 | SR-4370 is a potent and selective inhibitor of class I HDACs with IC50 of 0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM for HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6, respectively.SR-4370 suppresses AR signaling and in vivo prostate tumor growth. | ||
| E7481 | Givinostat | Givinostat is an orally active, hydroxamic acid-containing inhibitor of histone deacetylases (HDACs), with the potential to treat children with systemic juvenile idiopathic arthritis. It primarily targets Class I and II HDACs, with IC50 of 198 nM and 157 nM for HDAC1 and HDAC3, respectively. | ||
| S1313 | GSK3117391 | GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor. | ||
| S8769 | Tinostamustine(EDO-S101) | Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs). | ||
| S8323 | ITSA-1 (ITSA1) | ITSA-1 (ITSA1) affects HDAC activity after TSA treatment but shows no activity towards other HDAC inhibitors. | ||
| S7617 | Tasquinimod | Tasquinimod (ABR-215050) is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3. |
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| E6577New | 1-Naphthohydroxamic acid | 1-ナフトヒドロキサム酸（化合物2）は、IC50が14 μMの強力かつ選択的なHDAC8阻害剤です。1-ナフトヒドロキサム酸は、クラスIのHDAC1およびクラスIIのHDAC6（IC50 >100 μM）よりもHDAC8に対して選択性が高いです。1-ナフトヒドロキサム酸は、グローバルなヒストンH4のアセチル化を増加させず、また細胞内の総HDAC活性を低下させません。1-ナフトヒドロキサム酸はチューブリンのアセチル化を誘導することができます。 | ||
| E5952New | PT 3 | PT 3 is a benzamide-class, potent, and selective inhibitor of Histone Deacetylase 3 (HDAC3) with an IC50 of 245 nM. It crosses the blood-brain barrier and enhances learning and memory in novel object recognition models in mice. | ||
| E8292New | GEM144 | GEM144 is a potent and orally active dual inhibitor of DNA polymerase α (POLA1) and HDAC11 . It exhibits potent antiproliferative activity in vitro and antitumor efficacy in vivo by inducing p53 acetylation, p21 activation, G1/S cell cycle arrest, and apoptosis. | ||
| E5948New | PB94 | PB94 is a potent and selective inhibitor of HDAC11 with an IC50 of 108 nM and exhibits >40-fold selectivity over other HDAC isoforms. It ameliorates neuropathic pain in mouse models and can be radiolabeled with carbon-11 as [¹¹C]PB94 for PET imaging, demonstrating significant brain uptake and potential for in vivo imaging applications. | ||
| E5936New | FT895 | FT895は、IC50が3 nMの強力かつ選択的なHDAC11阻害剤です。 |
HDAC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