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GSK2636771
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GSK2636771
CAS No. : 1372540-25-4
MCE 站:GSK2636771
产品活性:GSK2636771 是一种口服有效的选择性 PI3Kβ 抑制剂,Ki和IC50分别为0.89,5.2 nM,比p110α和p110γ的选择性高900倍,比p110δ同种型的选择性高10倍。
研究领域:PI3K/Akt/mTOR
作用靶点:PI3K
In Vitro: GSK2636771 treatment causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells. Inhibition of p110β by GSK2636771 or AZD6482 leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines, whereas only marginal effects on AKT activation are observed in EEC cells.
In Vivo: GSK2636771 is a p110β inhibitor, and the p110β primes cells for response to growth factor stimulation. While p110β inhibition suppresses cell and tumor growth, dual targeting of p110α/β enhances apoptosis and provides sustained tumor response in mice model.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | 3-Methyladenine | LY294002 | Wortmannin | Quercetin | 740 Y-P | PI-103 | Isorhamnetin | Recilisib | Autophinib | AZD 6482 | PI3K-IN-1 | TG100-115 | α-Linolenic acid | TGX-221 | 1-Deoxynojirimycin | YS-49 | AS-605240 | PKI-402 | Disitertide | Erucic acid | CNX-1351 | GSK1059615 | Sonolisib | 1,3-Dicaffeoylquinic acid | GNE-317 | Esculetin | HS-173 | Oroxin B
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