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HJB97 可用于开发设计 PROTAC BET 的降解剂,具有抗肿瘤活性。HJB97 是高亲和力的 BET 抑制剂,Ki 值分别为 0.9 nM (BRD2 BD1),0.27 nM (BRD2 BD2),0.18 nM (BRD3 BD1),0.21 nM (BRD3 BD2),0.5 nM (BRD4 BD1),1.0 nM (BRD4 BD2)。
HJB97 可用于开发设计 PROTAC BET 的降解剂,具有抗肿瘤活性。HJB97 是高亲和力的 BET 抑制剂,Ki 值分别为 0.9 nM (BRD2 BD1),0.27 nM (BRD2 BD2),0.18 nM (BRD3 BD1),0.21 nM (BRD3 BD2),0.5 nM (BRD4 BD1),1.0 nM (BRD4 BD2)。
产品描述 | HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively). |
靶点活性 | BRD4 BD2:1.0nM, BRD4 BD2:7.0nM, BRD3 BD1:0.18nM, BRD3 BD1:6.6nM, BRD2 BD1:0.9(ki), BRD2 BD1:3.1nM, BRD3 BD2:0.21nM, BRD3 BD2:1.9nM, BRD2 BD2:0.27nM(ki), BRD2 BD2:3.9nM, Plusmn:0.01 nM (ki), Plusmn:0.03 nM (ki), Plusmn:0.09 nM (ki), Plusmn:0.1 nM (ki), Plusmn:0.2 nM, Plusmn:0.2 nM (ki), Plusmn:0.4 nM, Plusmn:0.5 nM, Plusmn:0.6 nM, Plusmn:0.7 nM, BRD4 BD1:0.5nM, BRD4 BD1:7.0nM |
体外活性 | HJB97是一种高效的额外末端(BET)抑制剂,具有极低的半抑制浓度(IC50,分别为BRD2 BD1的3.1 nM、BRD2 BD2的3.9 nM、BRD3 BD1的6.6 nM、BRD3 BD2的1.9 nM、BRD4 BD1的7.0 nM、BRD4 BD2的7.0 nM)。在RS4;11细胞系中,HJB97能够在300-1000 nM浓度下显著降低c-Myc水平(处理24小时)。此外,HJB97在10-1000 nM浓度范围内,经过4天的处理,有效抑制RS4;11和MOLM-13急性白血病细胞系的增长(IC50分别为24.1 nM和25.6 nM)。 |
分子量 | 500.55 |
分子式 | C26H28N8O3 |
CAS No. | 2093391-24-1 |
Smiles | CCn1nc(cc1Nc1nc(nc2[nH]c3cc(-c4c(C)noc4C)c(OC)cc3c12)C(=O)NC)C1CC1 |
密度 | 1.52 g/cm3 (Predicted) |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 27.0 mg/mL (53.9 mM), Sonication is recommended. H2O: insoluble | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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