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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
GSK690693, 蛋白激酶 C (PKC) 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Novel ATP-competitive pan-Akt kinase inhibitor.
GSK690693 has been used in western blotting and immunoprecipitations.
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%
规格
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
规格或纯度
Moligand™, 10mM in DMSO
英文名称
GSK690693
生化机理
GSK690693 是一种针对 Akt1/2/3 的泛 Akt 抑制剂，在无细胞试验中的 IC50 为 2 nM/13 nM/9 nM，对 AGC 激酶家族也很敏感：PKA、PrkX 和 PKC 同工酶敏感。GSK690693 还能有效抑制 CAMK 家族的 AMPK 和 DAPK3，IC50 分别为 50 nM 和 81 nM。GSK690693 会影响 Unc-51-like 自噬激活激酶 1 (ULK1) 的活性，并能强效抑制 STING 依赖性 IRF3 激活。第 1 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
蛋白激酶 C (PKC) 抑制剂
名称和识别符
EC号
804-554-1
分子类型
小分子
Isomeric SMILES
CCN1C2=C(C(=NC=C2OC[C@H]3CCCNC3)C#CC(C)(C)O)N=C1C4=NON=C4N
分子量
425.48
Reaxy-Rn
15495142
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15495142&ln=
技术文档
高级数据
产品属性
| ALogP | 0.3 |
|---|
关联靶点（人）
DCTPP1
Tchem
dCTP焦磷酸酶1(dCTP pyrophosphatase 1)
(1 活性数据)
PAK5
Tchem
丝氨酸/苏氨酸蛋白激酶 PAK 5(Serine/threonine-protein kinase PAK 5)
(2 活性数据)
PRKX
Tchem
cAMP依赖性蛋白激酶催化亚基PRKX(cAMP-dependent protein kinase catalytic subunit PRKX)
(3 活性数据)
PRKAR2A
Tchem
cAMP 依赖性蛋白激酶 II 型-α 调节亚基(cAMP-dependent protein kinase type II-alpha regulatory subunit)
(1 活性数据)
PRKACB
Tchem
cAMP 依赖性蛋白激酶催化亚基 β(cAMP-dependent protein kinase catalytic subunit beta)
(1 活性数据)
PRKG1
Tchem
cGMP依赖性蛋白激酶1(cGMP-dependent protein kinase 1)
(1 活性数据)
PRKG2
Tchem
cGMP依赖性蛋白激酶2(cGMP-dependent protein kinase 2)
(1 活性数据)
PRKCD
Tclin
蛋白激酶 C δ 型(Protein kinase C delta type)
(1 活性数据)
PRKCB
Tchem
蛋白激酶Cβ型(Protein kinase C beta type)
(1 活性数据)
PRKCE
Tchem
蛋白激酶 C ε 型(Protein kinase C epsilon type)
(2 活性数据)
PRKCH
Tchem
蛋白激酶Ceta型(Protein kinase C eta type)
(2 活性数据)
AKT3
Tchem
RAC-γ 丝氨酸/苏氨酸蛋白激酶(RAC-gamma serine/threonine-protein kinase)
(5 活性数据)
AKT2
Tchem
RAC-β丝氨酸/苏氨酸蛋白激酶(RAC-beta serine/threonine-protein kinase)
(6 活性数据)
AKT1
Tchem
RAC-alpha 丝氨酸/苏氨酸蛋白激酶(RAC-alpha serine/threonine-protein kinase)
(10 活性数据)
PRKAG2
Tchem
5'-AMP活化蛋白激酶亚基γ-2(5'-AMP-activated protein kinase subunit gamma-2)
(1 活性数据)
PAK4
Tchem
丝氨酸/苏氨酸蛋白激酶PAK 4(Serine/threonine-protein kinase PAK 4)
(3 活性数据)
PAK6
Tchem
丝氨酸/苏氨酸蛋白激酶 PAK 6(Serine/threonine-protein kinase PAK 6)
(3 活性数据)
PRKACA
Tchem
cAMP 依赖性蛋白激酶催化亚基 α(cAMP-dependent protein kinase catalytic subunit alpha)
(1 活性数据)
PRKCQ
Tchem
蛋白激酶Cθ型(Protein kinase C theta type)
(4 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (354.3 mM);
安全和危险性（GHS）
信号词
危险
危险声明
H301: 吞咽会中毒
WGK Germany
3
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
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