A selective PDK1 inhibitor
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GSK2334470

Item No. 18095

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
CAS Number
1227911-45-6
Molecular Formula
C25H34N8O
Formula Weight
462.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
226, 258, 328 nm
SMILES
NC1=NNC2=CC(C3=CC(N4C[C@@H](C(NC5CCCCC5)=O)CC[C@H]4C)=NC(NC)=N3)=CC=C21
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $84

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    10 mg

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    25 mg

    $369

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    50 mg

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    Product Description

    3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that plays an important role in growth factor signaling by phosphorylating and activating a group of kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. GSK2334470 is an inhibitor of PDK1 (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members.1 In HEK293 cells, 30 nM - 1 µM GSK2334470 suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well as the activation of Akt.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Najafov, A., Sommer, E.M., Axten, J.M., et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem. J. 433(2), 357-369 (2011).