GSK2334470 , 98% , 1227911-45-6

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

CAS NO.：1227911-45-6

Empirical Formula: C25H34N8O

Molecular Weight: 462.59

MDL number: MFCD21608525

PRODUCT Properties

• Density: 1.30±0.1 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO: ≥10mg/mL
• pka: 12.84±0.40(Predicted)
• form: powder
• color: white to light brown
• Stability: Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
• InChIKey: QLPHOXTXAKOFMU-WBVHZDCISA-N
• SMILES: N1(C2C=C(C3=CC4=C(C=C3)C(N)=NN4)N=C(NC)N=2)[C@H](C)CC[C@H](C(NC2CCCCC2)=O)C1

Description and Uses

GSK2334470 (1227911-45-6)?is a potent (IC50?= 10 nM) and selective inhibitor of 3-Phosphoinositide-dependent kinase 1 (PDK1), which phosphorylates and activates a group of protein kinases in the AGC/PKG/PKC family.1?It is more effective at inhibiting PDK1 substrates that are activated in the cytosol rather than at the plasma membrane.1?GSK2334470 delayed melanogenesis and metastasis in Braf(V600E)::Pten(-/-)?mice.2?It also displays antitumor activity against multiple myeloma synergistically with mTORC1/2 inhibitor PP2423?and proteasome inhibitor MG-1324.

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

Safety

• WGK Germany: 3