Cat. No. Name Size Price Add Cart
KI1095BX-9122 mg$144
BX-9125 mg$220
BX-91225 mg$650
BX-912100 mg$1650

Chemical Characteristic

Product NameBX-912
CAS No.702674-56-4
Molecular Weight 471.35
FormulaC20H23BrN8O
Chemical NameN-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
SmilesN1(CCCC1)C(=O)Nc1cc(ccc1)Nc1nc(c(cn1)Br)NCCc1nc[nH]c1
Chemical Structure

Biological activities

BX-912 is a selective and potent PDK1 inhibitor with an IC50 of 12 nM. BX-912 also inhibits ChcK1, PKA, CDK2, c-kit, and KDR with IC50 of 0.83, 0.11, 0.65, 0.85, and 0.41 µM, resepectively. BX-912 blocks PDK1/Akt signaling in PC-3 prostate cancer cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis. A number of cancer cell lines (including MDA-468 breast cancer cells) with elevated Akt activity show >30-fold more sensitive to growth inhibition by BX-912 in soft agar than on tissue culture plastic. BX-912 promotes a pronounced increase in the population of MDA-468 cells with 4 N DNA content. In addition, BX-912 potently inhibits the growth of HCT-116 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 µM. BX912 potently inhibits the growth of U87-MG glioblastoma cancer cells in soft agar, displaying an IC50 of 3.2 µM.[1] Furthermore, BX-912 significantly impairs MALT1 protease activity selectively in HBL1 and TMD8 cells.[2]

Protocols

In vitro: BX-912 is dissolved in DMSO.[2]

References

[1] Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005, 280(20): 19867-19874.
[2] Kloo B, et al. Critical role of PI3K signaling for NF-kappaB-dependent survival in a subset of activated B-cell-like diffuse large B-cell lymphoma cells. Proc Natl Acad Sci U S A. 2011, 108(1):272-277.

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