CID755673

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

第一个有效的、选择性的细胞活性泛 PKD 抑制剂。

The first potent and selective cell-active pan-PKD inhibitor with IC50s of 182/280/227 nM for PKD1/2/3 respectively; exhibits selectivity for PKD1 versus AKT, PLK1, CAK, CAMKIIα and three PKC isoforms; blockes phorbol ester-induced endogenous PKD1 activation in LNCaP cells and inhibits prostate cancer cell proliferation, cell migration and invasion.

CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 inhibits the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate cancer cell proliferation, cell migration, and invasion.

Acute administration of the PKD inhibitor CID755673 to normal mice reduces both PKD1 and 2 phosphorylation in a time and dose-dependent manner. Chronic CID755673 administration to T2D db/db mice for two weeks reduces expression of the gene expression signature of PKD activation, enhances indices of both diastolic and systolic left ventricular function and is associated with reduced heart weight.

CID 755673 | CID-755673

Apoptosis

PKD

PKD1|PKD2|PKD3

Cancer

——

521937-07-5

217.2206

C12H11NO3

>98% (HPLC)

DMSO: ≥ 40 mg/mL

O=C1NCCCC2=C1OC3=CC=C(O)C=C32

1H-Benzofuro[2,3-c]azepin-1-one, 2,3,4,5-tetrahydro-7-hydroxy-

(-20℃)

With Ice Pack

≥ 2 years