A potent inhibitor of PDK1
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BX-912

Item No. 14708

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-bromo-4-[[2-(1H-imidazol-5-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
CAS Number
702674-56-4
Molecular Formula
C20H23BrN8O
Formula Weight
471.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 5 mg/mlEthanol: 5 mg/ml
λmax
238, 274 nm
SMILES
BrC1=CN=C(N=C1NCCC2=CN=CN2)NC3=CC(NC(N4CCCC4)=O)=CC=C3
InChi Code
InChI=1S/C20H23BrN8O/c21-17-12-24-19(28-18(17)23-7-6-16-11-22-13-25-16)26-14-4-3-5-15(10-14)27-20(30)29-8-1-2-9-29/h3-5,10-13H,1-2,6-9H2,(H,22,25)(H,27,30)(H2,23,24,26,28)
InChi Key
DMMILYKXNCVKOJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM).1 It less effectively inhibits a panel of related serine-threonine kinases.1 BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Feldman, R.I., Wu, J.M., Polokoff, M.A., et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. The Journal of Biological Chemisty 280(20), 19867-19874 (2005).

    2. Kloo, B., Nagel, D., Pfeifer, M., et al. Critical role of PI3K signaling for NF-κB-dependent survival in a subset of activated B-cell-like diffuse large B-cell lymphoma cells. Proc. Natl. Acad. Sci. USA 108(1), 272-277 (2011).

    3. Mashukova, A., Forteza, R., Wald, F.A., et al. PDK1 in apical signaling endosomes participates in the rescue of the polarity complex atypical PKC by intermediate filaments in intestinal epithelia. Mol. Biol. Cell 23(9), 1664-1674 (2012).

    4. Shibata, E., Kanno, T., Tsuchiya, A., et al. Free fatty acids inhibit protein tyrosine phosphatase 1B and activate Akt. Cell. Physiol. Biochem. 32(4), 871-879 (2013).