LY294002

製品コードS1105 バッチS110509

印刷

化学情報

Chemical Structure Synonyms SF 1101, NSC 697286 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H17NO3
分子量 307.34 CAS No. 154447-36-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 31 mg/mL (100.86 mM)
Ethanol 15 mg/mL (48.8 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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。
in vitro

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1[5]. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
in vivo

LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]

プロトコル(参考用のみ)

キナーゼアッセイ kinase assays
PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.
細胞アッセイ 細胞株 Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
濃度 0–50 μM
反応時間 0–48 hours
実験の流れ

1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.
動物実験 動物モデル Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
投薬量 0–100 mg/kg
投与方法 Administered via i.p.

カスタマーフィードバック

Data from [Data independently produced by Int J Biochem Cell Biol, 2015, 60, 34-42]

Data from [Data independently produced by Hum Reprod, 2015, 30(2), 284-98]

Data from [Data independently produced by Sci Rep, 2015, 5, 11634]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Non-catalytic role of phosphoinositide 3-kinase in mesenchymal cell migration through non-canonical induction of p85β/AP2-mediated endocytosis [ Nat Commun, 2024, 15(1):2612] PubMed: 38521786
PD-L1-expressing tumor-associated macrophages are immunostimulatory and associate with good clinical outcome in human breast cancer [ Cell Rep Med, 2024, 5(2):101420] PubMed: 38382468
Tumor suppressor let-7 acts as a key regulator for pluripotency gene expression in Muse cells [ Cell Mol Life Sci, 2024, 81(1):54] PubMed: 38261036
Subtle structural alteration in indisulam switches the molecular mechanisms for the inhibitory effect on the migration of gastric cancer cells [ Biomed Pharmacother, 2024, 172:116259] PubMed: 38359488
Autophagy is essential for human myelopoiesis [ Stem Cell Reports, 2024, 19(2):196-210] PubMed: 38215759
FGF17 protects cerebral ischemia reperfusion-induced blood-brain barrier disruption via FGF receptor 3-mediated PI3K/AKT signaling pathway [ Eur J Pharmacol, 2024, 971:176521] PubMed: 38522639
NOP14-mediated ribosome biogenesis is required for mTORC2 activation and predicts rapamycin sensitivity [ J Biol Chem, 2024, S0021-9258(24)00057-7] PubMed: 38272224
Large-scale generation of IL-12 secreting macrophages from human pluripotent stem cells for cancer therapy [ Mol Ther Methods Clin Dev, 2024, 32(1):101204] PubMed: 38390556
Ursolic acid inhibits the metastasis of colon cancer by downregulating ARL4C expression [ Oncol Rep, 2024, 51(2)27] PubMed: 38131251
Pulsatilla saponin D regulates ras-related C3 botulinum toxin substrate 3 (RAC3) to overcome resistance to paclitaxel in lung adenocarcinoma cells [ BMC Cancer, 2024, 24(1):55] PubMed: 38200409

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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