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CAS No. : 1056901-62-2
MCE 国际站:AT13148
产品活性:AT13148 是一种可口服的,ATP 竞争性的 AGC kinase 的抑制剂,能够抑制 Akt1/Akt2/Akt3,p70S6K,PKA 和 ROCKI/ROCKII 的活性,IC50 值分别为 38 nM/402 nM/50 nM,8 nM,3 nM 和 6 nM/4 nM。
研究领域:PI3K/Akt/mTOR | Stem Cell/Wnt | Cell Cycle/DNA Damage | TGF-beta/Smad | Cytoskeleton | MAPK/ERK Pathway
作用靶点:Akt | PKA | ROCK | Ribosomal S6 Kinase (RSK)
In Vitro: AT13148 inhibits a panel of kinases at 10 μM, and the IC50 values for p70S6K, PKA, ROCKI, and ROCKII are all less than 10 nM and those for AKT1, 2, and 3 are 38, 402, and 50 nM, respectively. For the related AGC kinases RSK1 and SGK3, the IC50 values are 85 and 63 nM, respectively. In contrast, IC50 values for the non-AGC kinases CHK2 and Aurora B are both greater than 800 nM. AT13148 potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines. AT13148 treatment in gastric cancer cells dramatically suppresses activation of multiple AGC kinases, including Akt (at p-Thr-308), p70S6 kinase (p70S6K), glycogen synthase kinase 3β (GSK-3β) and p90 ribosomal S6 kinase (RSK).
In Vivo: Oral drug administration of 5 mg/kg of AT13148 results in complete bioavailability. Clear inhibition of phosphorylation of the AKT substrates GSK3β, tuberin, and the p70S6K target S6RP are also observed in PTEN-deficient MES-SA human uterine tumor xenografts after treatment with 40 and 50 mg/kg p.o. of AT13148. Oral gavage of AT13148 at well-tolerated doses significantly inhibits HGC27 xenograft tumor growth in nude mice. AGC activity is also dramatically decreased in AT13148-administrated HGC27 tumors.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | MAPK Compound Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Glucose Metabolism Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Staurosporine | LM22B-10 | SL 0101-1 | Insulin Detemir | (rac)-AG-205 | Rp-cAMPS | Cys-Kemptide | Multi-kinase-IN-2 | Akt/SKG Substrate Peptide | Chroman 1 dihydrochloride | AS1949490 | RSK2-IN-3 | 1,3-Dicaffeoylquinic acid | Ripasudil free base | Threo-Chloramphenicol-d6 | AKT-IN-14 | NSC45586 | APN/AKT-IN-1 | MS5033 | AS1892802 | Sophocarpine monohydrate | MS143 | Deferoxamine | Chaetominine | Hu7691 free base | AKT-IN-3 | 8-Aminoadenosine | Nrf2/HO-1 activator 2 | Sovesudil
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货号: HY-16071
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