CID755673是高效选择性的PKD1抑制剂，IC₅₀ of 值为182 nM。

CID755673 is a potent PKD inhibitor with IC 50 s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

Solid

PKD1 182 nM (IC50) PKD3 227 nM (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Sharlow ER, et al. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov 28;283(48):33516-26.
[2]. Venardos K, et al. The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. PLoS One. 2015 Mar 23;10(3):e0120934.

In Vitro: DMSO : 100 mg/mL (460.36 mM; Need ultrasonic)配制储备液