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BG45
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。
BG45图片
CAS NO:926259-99-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
BG45 是一种 HDAC I 类抑制剂,对 HDAC3 具有选择性 (IC50 = 289 nM)。
Cas No.926259-99-6
化学名(Z)-N-(2-aminophenyl)pyrazine-2-carbimidic acid
Canonical SMILESNC1=CC=CC=C1/N=C(O)/C2=CN=CC=N2
分子式C11H10N4O
分子量214.22
溶解度DMF: 5 mg/ml,DMSO: 30 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 3 mg/ml
储存条件Store at -20℃
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

Description:

IC50: 289 nM

Histone deacetylases (HDACs) represent novel molecular targets for the treatment of various types of cancers including multiple myeloma (MM). Many HDAC inhibitors have already shown remarkable anti-tumor activities in the preclinical studies, however, their clinical utility is limited due to unfavorable toxicities associated with their broad range HDAC inhibitory effects. BG45 is a novel small molecule HDAC3-selective inhibitor.

In vitro: BG45 is reported as an HDAC class I inhibitor with selectivity for HDAC3 over HDAC1, 2. Consistent with HDAC3 knockdown data, BG45 significantly inhibited MM cell growth dose-dependently. Importantly, BG45 also triggered a potent growth inhibitory effect against patient-derived MM cells, without affecting normal donor PBMCs [1].

In vivo: BG45 significantly inhibited MM tumor growth in a dose-dependent fashion. For example, significant differences were observed in control versus BG45 15 mg/kg, control versus BG45 50 mg/kg, and BG45 15 mg/kg versus BG45 50 mg/kg at day 22. Moreover, BG45 50 mg/kg in combination with bortezomib enhanced either single agent activity further. These results confirmed that BG45 triggers in vivo anti-MM activities [1].

Clinical trial: Up to now, BG45 is still in the preclinical development stage.

Reference:
[1] Minami J, Suzuki R, Mazitschek R, Gorgun G, Ghosh B, Cirstea D, Hu Y, Mimura N, Ohguchi H, Cottini F, Jakubikova J, Munshi NC, Haggarty SJ, Richardson PG, Hideshima T, Anderson KC.  Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9.