521937-07-5CID 755673

产品属性：

Cas No.521937-07-5

别名

化学名 7-hydroxy-2,3,4,5-tetrahydro-[1]benzofuro[2,3-c]azepin-1-one

分子式 C12H11NO3

分子量 217.22

溶解度 ≥ 5.55mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
CID755673, benzoxoloazepinolone, is the first identified cell-active small molecule PKD antagonist. It inhibits the activity of PKD1 with an IC50 of 182 nM and demonstrates highest selectivity to PKD1 when compared with AKT, PLK1, CAK, CAMKIIα, PKD2 and PKD3. Moreover, it was not competitive with ATP for enzyme inhibition. [1]

In vitro: In cell based assays, CID755673 dose-dependently suppressed PKD1 activation induced by phorbol ester endogenous in LNCaP cells. It was also reported to reverse biological actions of PKD1 including class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis, virus glycoprotein delivery from the Golgi to the plasma membrane as well as the ilimaquinone-induced Golgi fragmentation. Moreover, CID755673 suppressed prostate cancer cell proliferation, cell migration, and invasion. [1]

In vivo: Experimental models of acute pancreatitis were developed to study the effect of CID755673 on acute pancreatitis in vivo. Results demonstrated that this compound suppressed PKD1/2 and therefore significantly offset necrosis and severity of pancreatitis. [2]

Clinical trial: So far, no clinical trial has been conducted.

References:

[1]Sharlow ER, Giridhar KV, LaValle CR, Chen J, Leimgruber S, Barrett R, Altamirano KB, Wipf P, Lazo JS and Wang QJ.  Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov. 283(48): 3351246.

[2]Yuan JZ, Liu YN, Tan TY, Guha S, Gukovsky I, Gukovskaya A and Pandol SJ.  Protein kinase D regulates cell death pathways in experimental pancreatitis. Front Physiol. 2012 Mar. 3: DOI: 10.3389/fphys.2012.00060.