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HJB97
Catalog No. T15484Cas No. 2093391-24-1
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).
HJB97
Catalog No. T15484Cas No. 2093391-24-1
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).
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Product Introduction
Bioactivity
Chemical Properties
| 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 | 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 |
| 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 & Solubility Information
| 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 | |||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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