HJB97 |
| Catalog No.GC33211 |
HJB97 est un inhibiteur BET de haute affinité avec Kis de 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), respectivement. HJB97 est utilisé pour la conception d'un dégradeur potentiel de PROTAC BET et a une activité antitumorale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2093391-24-1
Sample solution is provided at 25 µL, 10mM.
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HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader. Antitumor activity[1].
HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC50s of 3.1±0.7 nM (BRD2 BD1), 3.9±0.5 nM (BRD2 BD2), 6.6±0.2 nM (BRD3 BD1), 1.9±0.4 nM (BRD3 BD2), 7.0±0.6 nM (BRD4 BD1), 7.0±0.1 nM (BRD4 BD2)[1].HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines with IC50s of 24.1±5.3 nM and 25.6±1.9 nM[1].HJB97 can effectively down-regulate the level of c-Myc at concentrations of 300-1000 nM in the RS4;11 cell line (treated for 24 h)[1].|| Cell Viability Assay[1]||Cell Line:|The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 cell line|Concentration:|10-1000 nM|Incubation Time:|4 days|Result:|Achieved IC50s value of 24.1±5.3 nM and 25.6±1.9 nM in inhibition of the RS4;11 cell and MOLM-13 cell growth.|| Western Blot Analysis[1]||Cell Line:|RS4;11 cells |Concentration:|30, 100, 300, 1000 nM|Incubation Time:|24 h|Result:|Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11 cell line.
[1]. 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.
| Cas No. | 2093391-24-1 | SDF | |
| Canonical SMILES | O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NC | ||
| Formula | C26H28N8O3 | M.Wt | 500.55 |
| Solubility | DMSO : 30 mg/mL (59.93 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9978 mL | 9.989 mL | 19.978 mL |
| 5 mM | 0.3996 mL | 1.9978 mL | 3.9956 mL |
| 10 mM | 0.1998 mL | 0.9989 mL | 1.9978 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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