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SML0217

Sigma-Aldrich

GSK2334470

≥98% (HPLC)

Sinonimo/i:

(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

Formula empirica (notazione di Hill):
C25H34N8O
Numero CAS:
1227911-45-6
Peso molecolare:
462.59
Numero MDL:
MFCD21608525
Codice UNSPSC:
12352200
ID PubChem:
329825237
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to light brown

Solubilità

DMSO: ≥10 mg/mL

Temperatura di conservazione

2-8°C

Stringa SMILE

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
QLPHOXTXAKOFMU-WBVHZDCISA-N

Applicazioni

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

Azioni biochim/fisiol

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.

Altre note

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.

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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
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
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
Zhiyong Zhang et al.
Scientific reports, 9(1), 7020-7020 (2019-05-09)
TLR4 is implicated in diseases associated with chronic low-grade inflammation, yet homeostatic signaling mechanisms that prevent and/or are affected by chronic TLR4 activation are largely uncharacterized. We recently reported that LPS/TLR4 activates in human leukocytes signaling intermediates (SI), abbreviated TLR4-SI
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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