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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

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
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].
Chemical Properties
Molecular Weight500.55
FormulaC26H28N8O3
Cas No.2093391-24-1
Storage & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.9978 mL9.9890 mL19.9780 mL99.8901 mL
5 mM0.3996 mL1.9978 mL3.9956 mL19.9780 mL
10 mM0.1998 mL0.9989 mL1.9978 mL9.9890 mL
20 mM0.0999 mL0.4995 mL0.9989 mL4.9945 mL
50 mM0.0400 mL0.1998 mL0.3996 mL1.9978 mL

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