Shopping Cart
- Remove All
- Your shopping cart is currently empty
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).
Description | 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). |
Targets&IC50 | BRD2 BD1:0.9(ki), Plusmn:0.03 nM (ki), Plusmn:0.6 nM, BRD3 BD1:0.18nM, BRD2 BD2:3.9nM, Plusmn:0.4 nM, BRD3 BD1:6.6nM, Plusmn:0.01 nM (ki), Plusmn:0.5 nM, BRD4 BD2:1.0nM, BRD3 BD2:1.9nM, Plusmn:0.2 nM, BRD4 BD1:7.0nM, BRD2 BD1:3.1nM, Plusmn:0.09 nM (ki), Plusmn:0.7 nM, BRD3 BD2:0.21nM, Plusmn:0.1 nM (ki), BRD4 BD1:0.5nM, BRD4 BD2:7.0nM, BRD2 BD2:0.27nM(ki), Plusmn:0.2 nM (ki) |
In vitro | HJB97 is a highly potent BET inhibitor with IC50 values of 3.1 nM (BRD2 BD1), 3.9 nM (BRD2 BD2), 6.6 nM (BRD3 BD1), 1.9 nM (BRD3 BD2), and 7.0 nM for both BRD4 BD1 and BD2. At concentrations of 300-1000 nM, HJB97 effectively down-regulates c-Myc levels in RS4;11 cell lines within 24 hours. Additionally, HJB97 (10-1000 nM over 4 days) significantly inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines, with IC50 values of 24.1 nM and 25.6 nM, respectively[1]. |
Molecular Weight | 500.55 |
Formula | C26H28N8O3 |
Cas No. | 2093391-24-1 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 27.0 mg/mL (53.9 mM), Sonication is recommended. H2O: insoluble | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.