SML0217
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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关于此项目
经验公式（希尔记法）:
C25H34N8O
化学文摘社编号:
分子量:
462.59
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
GSK2334470, ≥98% (HPLC)
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
SMILES string
CNc1nc(cc(n1)-c2ccc3c(N)n[nH]c3c2)N4C[C@H](CC[C@H]4C)C(=O)NC5CCCCC5
InChI key
QLPHOXTXAKOFMU-WBVHZDCISA-N
assay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: ≥10 mg/mL
storage temp.
2-8°C
Quality Level
Application
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
Biochem/physiol Actions
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.
Other Notes
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Chunmei Yang et al.
Oncotarget, 8(24), 39185-39197 (2017-04-14)
A deeper understanding of the complex pathogenesis of multiple myeloma (MM) continues to lead to novel therapeutic approaches. Prior studies suggest that 3-phosphoinositide-dependent kinase 1 (PDK1) is expressed and active, acting as a crucial regulator of molecules that are essential
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
Laura C Hautala et al.
Cellular signalling, 28(10), 1463-1469 (2016-07-05)
Glycodelin is a glycoprotein mainly expressed in well-differentiated epithelial cells in reproductive tissues. In normal secretory endometrium, the expression of glycodelin is abundant and regulated by progesterone. In hormone-related cancers glycodelin expression is associated with well-differentiated tumors. We have previously
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