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SML0217

Sigma-Aldrich

GSK2334470

≥98% (HPLC)

Synonym(e):

(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

Empirische Formel (Hill-System):
C25H34N8O
CAS-Nummer:
1227911-45-6
Molekulargewicht:
462.59
MDL-Nummer:
MFCD21608525
UNSPSC-Code:
12352200
PubChem Substanz-ID:
329825237
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Farbe

white to light brown

Löslichkeit

DMSO: ≥10 mg/mL

Lagertemp.

2-8°C

SMILES String

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

InChIKey

QLPHOXTXAKOFMU-WBVHZDCISA-N

Anwendung

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. Wirkung

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 (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.

Sonstige Hinweise

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

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Danielle L Schmitt et al.
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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
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
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
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
Xiao Shi et al.
Molecular pharmacology, 96(4), 493-504 (2019-08-15)
Methamphetamine (MA) is highly addictive and neurotoxic, causing cell death in humans and in rodent models. MA, along with many of its analogs, is an agonist at the G protein-coupled trace amine-associated receptor 1 (TAAR1). TAAR1 activation protects against MA-induced
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