1054543-47-3Apoptozole

产品属性：

Cas No.1054543-47-3

别名 Apoptosis Activator VII

化学名 4-[[2-[3,5-bis(trifluoromethyl)phenyl]-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl]methyl]-benzamide

分子式 C33H25F6N3O3

分子量 625.6

溶解度 ≤10mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide

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：
Apoptozole is an inhibitor of ATPase activity of HSP70 [1].

The heat shock protein 70 (HSP70) protein family plays diverse roles in biological processes and has multiple functions involved in suppression of apoptotic pathways through multiple anti-apoptotic processes. The two major members, constitutive Hsc70 and inducible Hsp70, are composed of an N-terminal ATPase domain and a C-terminal substrate binding domain [1][2].

Apoptozole (Az) is an inhibitor of ATPase activity of HSP70. Apoptozole inhibited the ATPase activity of HSP70 by binding to its ATPase domain. In the presence of 200 μM ATP, Apoptozole inhibited the ATPase activity of HSP70 by 32% and 65% at 100 μM and 200 μM, respectively. Apoptozole bound HSP70 but not HSP40, HSP60, and HSP90. In several cancer cell lines, Apoptozole induced apoptosis in a dose-dependent way with IC50 values ranged from 5 to 7 μM. In HeLa cells, Apoptozole decreased the amount of APAF-1 associated with HSP70 without affecting the expression level of APAF-1, and produced cleaved procaspase-9, suggesting that Apoptozole blocked association of HSP70 with APAF-1 and induced caspase-dependent apoptosis.

In the nude mice xenografted with A549, RKO (colorectal carcinoma), and HeLa cells, i.p injection of Apoptozole reduced tumor volumes by 61%, 65%, and 68%, respectively [1]. In mice administered with both protein antigen and Az, Az increased immune responses to administered antigens and produced more antibodies [2].