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Safety Information

SML0217

Sigma-Aldrich

GSK2334470

≥98% (HPLC)

Synonym(s):

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

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5 MG
¥27,970
25 MG
¥70,210

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5 MG
¥27,970
25 MG
¥70,210

About This Item

Empirical Formula (Hill Notation):
C25H34N8O
CAS Number:
1227911-45-6
Molecular Weight:
462.59
MDL number:
MFCD21608525
UNSPSC Code:
12352200
PubChem Substance ID:
329825237
NACRES:
NA.77

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: ≥10 mg/mL

storage temp.

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

InChI key

QLPHOXTXAKOFMU-WBVHZDCISA-N

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[1]
  • glycodelin-transfected HEC-1B human endometrial adenocarcinoma cells.[2]
  • HeLa and Hs578T cells to test its effect on formylglycinamidine ribonucleotide synthase (FGAMS) assembly[3]

Biochem/physiol Actions

GSK2334470 (GSK-470) mediates cell cycle arrest. It also inhibits cellular proliferation and induces apoptosis in cancer cells.[4]
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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

SML0217-25MG:
SML0217-VAR:
SML0217-BULK:
SML0217-5MG:

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Certificates of Analysis (COA)

Lot/Batch Number
0000167604
053M4619V
121M4615V

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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
View All Related Papers

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