Structure
HJB97, inhibitor
HJB97
Purity
98.00%
Synonyms
HJB97; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 30mg/mL (59.93mM) Need ultrasonic
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
H2O: <0.1mg/mL (insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C26H28N8O3
SMILES
O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NC
CAS Number
2093391-24-1
Target & IC50
BRD2 BD1: ic50 3.1nM
plusmn: ic50 0.6nM
BRD2 BD2: ic50 3.9nM
BRD3 BD1: ic50 6.6nM
BRD3 BD2: ic50 1.9nM
BRD4 BD1: ic50 7.0nM
BRD4 BD2: ic50 7.0nM
plusmn: ic50 0.6nM
BRD2 BD2: ic50 3.9nM
BRD3 BD1: ic50 6.6nM
BRD3 BD2: ic50 1.9nM
BRD4 BD1: ic50 7.0nM
BRD4 BD2: ic50 7.0nM
In Vitro
HJB97 is a highly potent and extra terminal (BET) inhibitor (IC50s of 3.1nM (BRD2 BD1), 3.9nM (BRD2 BD2), 6.6nM (BRD3 BD1), 1.9nM (BRD3 BD2), 7.0nM (BRD4 BD1), 7.0nM (BRD4 BD2)). HJB97 can potently down-regulate the level of c-Myc at concentrations of 300-1000nM in the RS4;11 cell line (treated for 24 hours). HJB97 (10-1000nM, 4 days) effectively inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines (IC50s of 24.1nM and 25.6nM)[1].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for HJB97, inhibitor
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: 0.9nM (BRD2 BD1), 0.27nM (BRD2 BD2), 0.18nM (BRD3 BD1), 0.21nM (BRD3 BD2), 0.5nM (BRD4 BD1), 1.0nM (BRD4 BD2), respectively).
Product Categories/Family for HJB97, inhibitor
References
Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
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Product Notes
The HJB97 (Catalog #AAA5754961) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "HJB97, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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