货号	规格	价格	上海	北京	珠海	重庆	武汉
S81130-5mg促销	≥98%	￥618.00 ￥556.00 S81130-5mg ￥556.00 现货	5 5	-	-	-	-
S81130-10mg促销	≥98%	￥926.00 ￥832.00 S81130-10mg ￥832.00 现货	5 0 5	-	-	-	-
S81130-50mg促销	≥98%	￥3100.00 ￥2790.00 S81130-50mg ￥2790.00 现货	2 2	-	-	-	-
S81130-100mg促销	≥98%	￥5190.00 ￥4670.00 S81130-100mg ￥4670.00 现货	2 2	-	-	-	-

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产品描述：

GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation

靶点：

Akt1:2 nM (IC50);Akt3:9 nM (IC50);Akt2:13 nM (IC50);PKCη:2 nM (IC50);PKCθ:2 nM (IC50);PrkX:5 nM (IC50);PAK6:6 nM (IC50);PAK4:10 nM (IC50);PKCδ:14 nM (IC50);PKCβ1:19 nM (IC50);PKCε:21 nM (IC50);PKA:24 nM (IC50);PKG1β:33 nM (IC50);AMPK:50 nM (IC50);PAK5:52 nM (IC50);DAPK3:81 nM (IC50);Autophagy;SerineProtease; Akt; PKC; AMPK; Autophagy

体内研究：

A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day. GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt

参考文献：

1. Rhodes N, et al. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res, 2008, 68(7), 2366-2374. 2. Levy DS, et al. AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines. Blood, 2009, 113(8), 1723-1729. 3. Altomare DA, et al. GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt. Clin Cancer Res, 2010, 16(2), 486-496. 4. Konno H, et al. Pro-inflammation Associated with a Gain-of-Function Mutation (R284S) in the Innate Immune Sensor STING. Cell Rep. 2018 Apr 24;23(4):1112-1123.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.35 ml	11.751 ml	23.503 ml
5 mM	0.47 ml	2.35 ml	4.701 ml
10 mM	0.235 ml	1.175 ml	2.35 ml
50 mM	0.047 ml	0.235 ml	0.47 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献(1篇)

1. [IF=5.1] Cai Zhiqing et al."β-hydroxybutyrate ameliorates osteoarthritis through activation of the ERBB3 signaling pathway in mice."JOURNAL OF BONE AND MINERAL RESEARCH.2024 Nov;:

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GSK690693,新型ATP竞争性泛Akt激酶抑制剂

GSK690693

参考文献(1篇)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)