中文名:GSK690693
英文名:GSK690693
英文别名:4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-((S)-piperidin-3-ylmethoxy)-1H-imidazo[4,5-c]pyridin-4-yl)-2-methylbut-3-yn-2-ol
纯度:10mM in DMSO
货号:G409035
包装:1ml
Cas号:937174-76-0
存储温度:-80℃储存
产品介绍:
Information
GSK690693 is a pan-Akt inhibitor targetingAkt1/2/3withIC50of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibitsAMPKandDAPK3from the CAMK family with IC50 of 50 nM and
In vitro
GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50 of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50 of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50 ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations >100 nM in both LNCaP and BT474 cells. Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines.
In vivo
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.
Cell Data
cell lines:Ba/F3 cells expressing wild-type or mutant human Kit, HMC1, HMC-1α155
Concentrations:Dissolved in DMSO, final concentrations ~30 μM
Incubation Time:72 hours
Powder Purity:≥98%
查看阿拉丁官网此产品相关对应页面:https://www.aladdin-e.com/zh_cn/G409035.html
关键字: 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-((S)-piperidin-3-ylmethoxy)-1H-imidazo[4,5-c]pyridin-4-yl)-2-methylbut-3-yn-2-ol
上海阿拉丁生化科技股份有限公司是A股上市公司((股票代码:688179),专注于科研试剂的研发、生产和销售,已陆续建立多个工厂和研发中心。作为领军企业,阿拉丁始终坚持质量第一,连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种,SKU总数超过46万,产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域,是国内少数化学试剂到生物试剂全面发展的国产试剂品牌,产品同步发布在我们国内(www.aladdin-e.com)和海外(www.aladdinsci.com)电商平台。