HJB97 - Epigenetic Reader Domain 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHJB97Cat. No.: HY-112429CAS No.: 2093391-24-1分式: CHNO分量: 500.55作靶点: Epigenetic Reader Domain作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (59.93 mM; Need ultrason

2、ic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.99 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.99 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 HJB97种亲和 BET 抑制剂，Ki 值分别为 0.90.2 nM (BRD2 BD1)，0.270.09 nM

3、 (BRD2BD2)，0.180.01 nM (BRD3 BD1)，0.210.03 nM (BRD3 BD2)，0.50.2 nM (BRD4 BD1)，1.00.1 nM(BRD4 BD2)。HJB97 可于开发设计 PROTAC BET 的降解剂。具有抗肿瘤活性 1。IC50 & Target BRD2 BD1 BRD2 BD2 BRD3 BD1 BRD3 BD20.9 nM (Ki) 0.27 nM (Ki) 0.18 nM (Ki) 0.21 nM (Ki)BRD4 BD1 BRD4 BD2 BRD2 BD1 BRD2 BD20.5 nM (Ki) 1.0 nM (Ki) 3.1 n

4、M (IC50) 3.9 nM (IC50)BRD3 BD1 BRD3 BD2 BRD4 BD1 BRD4 BD26.6 nM (IC50) 1.9 nM (IC50) 7.0 nM (IC50) 7.0 nM (IC50)体外研究 HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC50s of3.10.7 nM (BRD2 BD1), 3.90.5 nM (BRD2 BD2), 6.60.2 nM (BRD3 BD1), 1.90.4 nM (BRD3 B

5、D2),7.00.6 nM (BRD4 BD1), 7.00.1 nM (BRD4 BD2) 1.HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lineswith IC50s of 24.15.3 nM and 25.61.9 nM 1.HJB97 can effectively down-regulate the level of c-Myc at concentrations of 300-1000 nM in the RS4;11 cel

6、lline (treated for 24 h) 1.Cell Viability Assay 1Cell Line: The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 celllineConcentration: 10-1000 nMIncubation Time: 4 daysResult: Achieved IC50s value of 24.15.3 nM and 25.61.9 nM in inhibition of the RS4;11 celland MOLM-13 cell g

7、rowth.Western Blot Analysis 1Cell Line: RS4;11 cellsConcentration: 30, 100, 300, 1000 nMIncubation Time: 24 hResult: Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11cell line.REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar CellularPotencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.McePdfHeightCaution: Product has not been fully validated for medical applications.For