化合物BG45 T2294

Product Introduction
Bioactivity


英文名: BG45

描述: BG45是一个 HDAC I 型抑制剂，选择性抑制 HDAC3，IC50为289 nM。它抑制 HDAC1/2/6的效力大大降低，IC50分别为2、2.2和>20μM。

细胞实验: The growth inhibitory effects of BG45 in MM cell lines are assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance. To measure proliferation of MM cells, the rate of DNA synthesis is measured by [3H]thymidine uptake.(Only for Reference)

激酶实验: Kinase assays: Initial rate constants are measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) are quenched with 20 μL Kinase-Glo detection buffer. Luminescence is detected in a plate-reading luminometer and the results are analyzed by nonlinear regression.

体外活性: BG45 causes significant cell growth inhibition and induces caspase-dependent apoptosis in a series of MM cells. In RPMI8226 cells, BG45 synergistically enhances bortezomib-induced cytotoxicity. [1]

体内活性: In mice bearing MM.1S xenograft of human MM, BG45 (50 mg/kg, i.p.) significantly inhibits MM tumor growth. When in combination with bortezomib, BG45 (50 mg/kg, i.p.) enhances bortezomib-induced cytotoxicity. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 2 mg/mL (9.33 mM)
DMSO : 39 mg/mL (182.1 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | inhibit | BG45 | HDAC | Histone deacetylases | BG 45 | BG-45 | Apoptosis

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相关库: Anti-Cancer Compound Library | NF-κB Signaling Compound Library | Inhibitor Library | Epigenetics Compound Library | Hematonosis Compound Library | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | Target-Focused Phenotypic Screening Library | Histone Modification Compound Library | Chromatin Modification Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途