产品属性：
产品名称 | 规格 | CAS号 | 型号 |
CID 755673 | 10mM (in 1mL DMSO) 5mg 10mg 50mg | 521937-07-5 | EY-Y0165520 |
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.
关键字： 521937-07-5;C12H11NO3;CID 755673;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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