HJB97 Inhibitor

Name: HJB97 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5754961
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754961

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),… More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Product Name

HJB97, Inhibitor

Full Product Name

HJB97

Product Gene Name

HJB97, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

500.55

Solubility

DMSO: 30mg/mL (59.93mM) Need ultrasonic
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

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].

Product Categories/Family for HJB97, inhibitor

Chromatin/Epigenetic; Epigenetic Reader Domain; Epigenetics

Product References and Citations for HJB97, inhibitor

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.

Other Notes

Small volumes of HJB97, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for HJB97 purchase

MBS5754961 is an inhibitor targeting HJB97.