HJB97
Based on 2 publication(s) in Google Scholar
HJB97 is a high-affinity BET inhibitor with Ki values of 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), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
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- Purity: 99.12%
- CAS No.: 2093391-24-1
- 화학식: C26H28N8O3
- 분자량:500.55
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) HJB97
More
Biological Activity
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BRD2 BD1 0.9±0.2 nM (Ki) |
BRD2 BD2 0.27±0.09 nM (Ki) |
BRD3 BD1 0.18±0.01 nM (Ki) |
BRD3 BD2 0.21±0.03 nM (Ki) |
BRD4 BD1 0.5±0.2 nM (Ki) |
BRD4 BD2 1.0±0.1 nM (Ki) |
BRD2 BD1 3.1±0.7 nM (IC50) |
BRD2 BD2 3.9±0.5 nM (IC50) |
BRD3 BD1 6.6±0.2 nM (IC50) |
BRD3 BD2 1.9±0.4 nM (IC50) |
BRD4 BD1 7.0±0.6 nM (IC50) |
BRD4 BD2 7.0±0.1 nM (IC50) |
BRD2 |
BRD3 |
BRD4 |
BET |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
25.6 nM
Compound: 8; HJB97
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Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
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[PMID: 28339196] |
| RS4-11 | IC50 |
24.1 nM
Compound: 8; HJB97
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Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
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[PMID: 28339196] |
HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC50s of 3.1 nM (BRD2 BD1), 3.9 nM (BRD2 BD2), 6.6 nM (BRD3 BD1), 1.9 nM (BRD3 BD2), 7.0 nM (BRD4 BD1), 7.0 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 nM and 25.6 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 cell line
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Concentration:10-1000 nM
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Incubation Time:4 days
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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.
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Cell Line:RS4;11 cells
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Concentration:30, 100, 300, 1000 nM
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Incubation Time:24 h
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Result:Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11 cell line.
Chemical Information
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CAS No. 2093391-24-1
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Appearance Solid
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분자량 500.55
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화학식 C26H28N8O3
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Color Light yellow to yellow
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SMILES
O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NC
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Pharmacol Transl Sci
General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex. [Abstract]2021 Feb 26;4(2):941-952. PMID: 33860212 -
용액&용해도
DMSO : 30 mg/mL (59.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (283 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Wang C, et al. PROTACs for BRDs proteins in cancer therapy: a review. J Enzyme Inhib Med Chem. 2022 Dec;37(1):1694-1703. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9978 mL | 9.9890 mL | 19.9780 mL | 49.9451 mL |
| 5 mM | 0.3996 mL | 1.9978 mL | 3.9956 mL | 9.9890 mL | |
| 10 mM | 0.1998 mL | 0.9989 mL | 1.9978 mL | 4.9945 mL | |
| 15 mM | 0.1332 mL | 0.6659 mL | 1.3319 mL | 3.3297 mL | |
| 20 mM | 0.0999 mL | 0.4995 mL | 0.9989 mL | 2.4973 mL | |
| 25 mM | 0.0799 mL | 0.3996 mL | 0.7991 mL | 1.9978 mL | |
| 30 mM | 0.0666 mL | 0.3330 mL | 0.6659 mL | 1.6648 mL | |
| 40 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL | 1.2486 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9989 mL |
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