化学性质:
规格 | 1mg 5mg |
CAS | 74 |
别名 |
|
化学名 | 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)isoxazole-3-carboxamide |
分子式 | C19H17ClN2O5 |
分子量 | 388.8 |
溶解度 | ≥ 38.9mg/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 |
产品描述:
VER-50589 is a potent inhibitor of HSP90 with IC50 value of 21 nM for HSP90β [1].
Heat shock protein 90 (HSP90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. Also, HSP90 stabilizes proteins required for tumor growth.
VER-50589 is a potent HSP90 inhibitor. VER-50589 inhibited recombinant yeast Hsp90 ATPase activity with IC50 value of 143 nM at 400 μM ATP and inhibited recombinant human HSP90β with IC50 value of 821 nM in the presence of the activator AHA1. Also, VER-50589 bound to recombinant human HSP90β with Kd value of 4.5 nM. In human cancer cells, VER-50589 exhibited antiproliferative activity with mean GI50 value of 78 nM. In CH1 human ovarian cells, VER-50589 inhibited cell growth with GI50 value of 32.7 nM. In HT29 cells, VER-50589 exhibited extensive glucuronidation and increased glucuronide levels by 50-fold, which were responsible for the resistance. In CH1doxR cells that were resistant to doxorubicin, VER-50589 exhibited similar cellular GI50 value compared with CH1 cells. In HCT116 colon cancer cells, VER-50589 caused G1 and G2-M block. Also, VER-50589 induced cytostasis and apoptosis [1].
In athymic mice bearing OVCAR3 human ovarian ascites tumors, VER-50589 completely inhibited HSP90. In mice bearing HCT116 colon carcinoma xenografts, VER-50589 (100 mg/kg) reduced tumor volume by 30% and tumor weight by 26%. Also, VER-50589 reduced expression of ERBB2 and C-RAF [1].
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
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