BX-912

Product NameBX-912
CAS702674-56-4
MFC20H23BrN8O
MW471.35
EINECS
MOL File702674-56-4.mol

Chemical Properties

Density	1.596
storage temp.	-20°C
solubility	≥23.55 mg/mL in DMSO; insoluble in H2O; ≥10.25 mg/mL in EtOH
form	powder
color	white to beige

Safety Information

WGK Germany

Usage And Synthesis

Description

3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC₅₀ = 26 nM). It less effectively inhibits a panel of related serine-threonine kinases. BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.

Uses

A selective potent PDK-1 inhibitor with an IC50 of 12 nM.

Uses

BX-912 is a selective potent 3-Phosphoinositide-dependent Kinase-1 (PDK1) inhibitor. BX-192 shows potential anticancer properties as it inibits PDK1 activity towards the signaling pathway in cancer cell growth, survival and tumor angiogenesis.

Definition

ChEBI: N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide is a member of ureas.

target

PDK-1

References

[1] feldman ri1, wu jm, polokoff ma, kochanny mj, dinter h, zhu d, biroc sl, alicke b, bryant j, yuan s, buckman bo, lentz d, ferrer m, whitlow m, adler m, finster s, chang z, arnaiz do. novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. j biol chem. 2005 may 20;280(20):19867-74. epub 2005 mar 16.