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J22352
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
J22352图片
CAS NO:2252395-44-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
J22352是一种具有类似靶向嵌合体蛋白水解(PROTAC)特性、高度选择性HDAC6抑制剂,其IC50值为4.7nM,J22352通过抑制胶质母细胞瘤自噬、诱发抗肿瘤免疫反应来促进HDAC6降解和诱导抗癌效果,并通过降低PD-L1的免疫抑制活性,使宿主抗肿瘤活性恢复。
Cas No.2252395-44-9
Canonical SMILESO=C(C1=CC=CC=C1N2CC3=CC=C(C(NO)=O)C=C3)N(CCC4=CC=CC=C4)C2=O
分子式C24H21N3O4
分子量415.44
溶解度DMSO: 125 mg/mL (300.89 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1[1]. HDAC6|4.7 nM (IC50)

J22352 (0.1-20 μM; 72 hours) decreases U87MG cell viability in a dose-dependent manner[1]. J22352 (10 μM; 24 hours) shows a dose-dependent decrease in HDAC6 protein abundance[1]. Cell Viability Assay[1] Cell Line: U87MG cells

J22352 (10mg/kg; given i.p. per day for 14 days in male nude mice) results in a >80% tumor growth inhibition (TGI) rate. J22352 is well tolerated in mice[1]. Animal Model: Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old)[1]

[1]. Liu JR, et al. High-selective HDAC6 inhibitor promotes HDAC6 degradation following autophagy modulation and enhanced antitumor immunity in glioblastoma. Biochem Pharmacol. 2019 May; 163:458-471.