| 名称 | LY-294002 hydrochloride |
| 描述 | LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation. |
| 细胞实验 | Cell lines: Colon cancer cell lines DLD-1,LoVo,HCT15,and Colo205. Concentrations: 0–50 μM. Incubation Time: 0–48 hours. Method: 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,Premix WST-1 (10 μL) is 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.[2] |
| 激酶实验 | 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 are established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.[4] |
| 动物实验 | Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p.with OVCAR-3 cells. Formulation: Dissolved in DMSO plus 0.25 ml of PBS. Dosages: 0–100 mg/kg. Administration: i.p.[3] |
| 体外活性 | LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. In these colon cancer cell lines, LY294002 shows a remarkable growth-inhibitory and apoptosis-inducing effect and decreases expression of phosphorylated Akt (Ser473)[2]. LY294002 induces diminished cytoplasmic volume and obvious nuclear pyknosis in the tumor cells. 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[3]. |
| 体内活性 | LY294002 can suppress tumor growth and induce apoptosis, especially in the LoVo tumors. Thus, It shows remarkable effectiveness in the mouse peritonitis carcinoma tosa model [2]. LY294002 markedly inhibits growth and ascites formation of ovarian carcinoma [3]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (145.43 mM)
Ethanol : 5 mM
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| 关键字 | Phosphoinositide 3-kinase | NPC | tumor | nuclear | DNA-PK | Casein Kinase | Inhibitor | PI3K | CNE-2Z | Human | inhibit | LY-294002 Hydrochloride | Lysophosphatidic acid | nasopharyngeal | DNA-dependent protein kinase | Leptin | NSC-697286 | LY294002 Hydrochloride | phosphatidylinositol 3-kinase | spermatozoa | broad-spectrum | translocation | SF1101 | LY 294002 hydrochloride | LY-294002 | SF-1101 | LY294002 | LY294002 hydrochloride | Apoptosis | NSC697286 | reversibly | carcinoma | LY 294002 Hydrochloride |
| 相关产品 | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | GDC0084 | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
| 相关库 | 抗胰腺癌化合物库 | 经典已知活性库 | HIF-1化合物库 | 激酶抑制剂库 | 抗卵巢癌化合物库 | 抑制剂库 | 代谢化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌活性化合物库 |
United States
