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Merck

SML0217

Sigma-Aldrich

GSK2334470

≥98% (HPLC)

别名:

(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide

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About This Item

经验公式(希尔记法):
C25H34N8O
分子量:
462.59
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

颜色

white to light brown

溶解性

DMSO: ≥10 mg/mL

储存温度

2-8°C

SMILES字符串

CNc1nc(cc(n1)-c2ccc3c(N)n[nH]c3c2)N4C[C@H](CC[C@H]4C)C(=O)NC5CCCCC5

InChI

1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1

InChI key

QLPHOXTXAKOFMU-WBVHZDCISA-N

应用

GSK2334470 has been used as an inhibitor of 3-phosphoinositide dependent protein kinase-1 (PDK-1) in:
  • Treg cells, to identify regulators of interleukin 2 (IL-2)– signal transducer and activator of transcription 5 (STAT5) signaling
  • glycodelin-transfected HEC-1B human endometrial adenocarcinoma cells.
  • HeLa and Hs578T cells to test its effect on formylglycinamidine ribonucleotide synthase (FGAMS) assembly

生化/生理作用

GSK2334470 (GSK-470) mediates cell cycle arrest. It also inhibits cellular proliferation and induces apoptosis in cancer cells.
GSK2334470 is a highly specific and potent inhibitor of PDK1
GSK2334470 is a highly specific and potent inhibitor of PDK1 (3-Phosphoinositide dependent protein kinase-1). GSK2334470 can be used in cells to ablate T-loop phosphorylation and activation SGK, S6K1 and RSK as well as suppress the activation of Akt.

其他说明

GSK2334470 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK2334470 probe summary on the Chemical Probes Portal website.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Chanyang Kim et al.
Endocrine connections, 7(3), 443-455 (2018-02-21)
Insulin-like growth factor (IGF)-1 is a well-known anti-apoptotic pro-survival factor and phosphatidylinositol-3-kinase (PI3K)/Akt pathway is linked to cell survival induced by IGF-1. It is also reported that Akt signaling is modulated by 3-phosphoinositide-dependent kinase-1 (PDK1). In the current study, we
Loka R Penke et al.
Scientific reports, 10(1), 1083-1083 (2020-01-25)
Interleukin (IL)-13 is a type 2 cytokine with important roles in allergic diseases, asthma, and tissue fibrosis. Its receptor (R) α1 is primarily responsible for the biological actions of this cytokine, while Rα2 possesses a decoy function which can block
Danielle L Schmitt et al.
PloS one, 13(4), e0195989-e0195989 (2018-04-19)
A macromolecular complex of the enzymes involved in human de novo purine biosynthesis, the purinosome, has been shown to consist of a core assembly to regulate the metabolic activity of the pathway. However, it remains elusive whether the core assembly
Nicola Michelle Bougen-Zhukov et al.
American journal of respiratory cell and molecular biology, 62(3), 331-341 (2019-09-13)
Hydrated magnesium silicate (or "talc" particles) is a sclerosis agent commonly used in the management of malignant pleural effusions, a common symptom of metastatic diseases, including lung cancers. However, the direct effects of talc particles to lung carcinoma cells, which
Cedric Leroy et al.
Breast cancer research : BCR, 18(1), 41-41 (2016-04-07)
The PI3K pathway is hyperactivated in many cancers, including 70 % of breast cancers. Pan- and isoform-specific inhibitors of the PI3K pathway are currently being evaluated in clinical trials. However, the clinical responses to PI3K inhibitors when used as single agents

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