BRD4 Inhibitor-20
Based on 1 publication(s) in Google Scholar
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.
For research use only. We do not sell to patients.
- Purity: 99.24%
- CAS No.: 2490311-14-1
- Formula: C18H18N2O4S
- Molecular Weight:358.41
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BRD4 Inhibitor-20
More
Biological Activity
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BRD4 BD1 19 nM (IC50) |
BRD4 BD2 28 nM (IC50) |
BRD2 (BD1) 24 nM (IC50) |
BRD2 (BD2) 18 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| GES1 | IC50 |
78.83 μM
Compound: XY-1
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Antiproliferative activity against human GES1 cells incubated for 72 hrs MTT assay
Antiproliferative activity against human GES1 cells incubated for 72 hrs MTT assay
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[PMID: 38749341] |
| HL-60 | IC50 |
1.35 μM
Compound: 12j
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Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay
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[PMID: 32883643] |
| HL-60 | IC50 |
14.16 μM
Compound: XY-1
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Antiproliferative activity against human HL-60 cells incubated for 72 hrs CCK-8 assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs CCK-8 assay
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[PMID: 38749341] |
| HT-29 | IC50 |
11.06 μM
Compound: XY-1
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Antiproliferative activity against human HT-29 cells incubated for 72 hrs MTT assay
Antiproliferative activity against human HT-29 cells incubated for 72 hrs MTT assay
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[PMID: 38749341] |
| HT-29 | IC50 |
4.75 μM
Compound: 12j
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Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay
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[PMID: 32883643] |
| MV4-11 | IC50 |
24.54 μM
Compound: XY-1
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Antiproliferative activity against human MV4-11 cells incubated for 72 hrs CCK-8 assay
Antiproliferative activity against human MV4-11 cells incubated for 72 hrs CCK-8 assay
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[PMID: 38749341] |
| WI-38 | IC50 |
44.07 μM
Compound: 12j
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Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay
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[PMID: 32883643] |
BRD4 Inhibitor-20 (compound 12j) exhibits excellent BRD4 inhibitory activities (BD1, IC50=19 nM; BD2, IC50=28 nM) and inhibitory activities against BRD2 (BD1, IC50=24 nM; BD2, IC50=18 nM)[1].
BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc[1].
BRD4 Inhibitor-20 (72 h) has anti-proliferation potency with IC50 values of 4.75 μM, 1.35 μM and 44.07 μM in HT-29, HL-60 and WI-38 cells, respectively[1].
BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:0.5, 2.5, 5.0 μM
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Incubation Time:24 h
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Result:Displayed profound inhibitory effects on c-Myc protein expression.
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Cell Line:HT-29, HL-60 and WI-38 cells
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Concentration:
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Incubation Time:72 h
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Result:Possessed strong anti-proliferative activity and weak toxicity.
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Cell Line:HT-29 cell lines
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Concentration:2.5, 5.0, 10.0 μM
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Incubation Time:24 h
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Result:Arrested the cell-cycle progression of the cell line into the G1 phases and the percentage of cells in G1 phase after treatment under concentrations of 2.5, 5.0 and 10.0 μM were 85.98%, 86.49% and 86.05%, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:rats[1]
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Dosage:5 mg/kg, 15 mg/kg
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Administration:intravenous dosing (iv) or oral dosing (po)
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Result:
PK Parameters iv (5 mg/kg) po (15 mg/kg) Cmax(μg/L) - 2175 Tmax(h) - 1.00 t1/2(h) 1.56 3.59 CLz/F (L/h/kg) 0.68 1.03 AUC0−t(μg/L*h) 7296 14384 AUC0−∞(μg/L*h) 7340 14600 F (%) - 66%
Chemical Information
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CAS No. 2490311-14-1
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Appearance Solid
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Molecular Weight 358.41
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Formula C18H18N2O4S
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Color Brown to reddish brown
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SMILES
O=C1NC2=CC=C(C=C2/C1=C(C)\C)NS(=O)(C3=C(C=CC=C3)OC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Bioorg Med Chem
2026 Jan 1:132:118483. PMID: 41240398
Solvent & Solubility
DMSO : 125 mg/mL (348.76 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7901 mL | 13.9505 mL | 27.9010 mL | 69.7525 mL |
| 5 mM | 0.5580 mL | 2.7901 mL | 5.5802 mL | 13.9505 mL | |
| 10 mM | 0.2790 mL | 1.3951 mL | 2.7901 mL | 6.9753 mL | |
| 15 mM | 0.1860 mL | 0.9300 mL | 1.8601 mL | 4.6502 mL | |
| 20 mM | 0.1395 mL | 0.6975 mL | 1.3951 mL | 3.4876 mL | |
| 25 mM | 0.1116 mL | 0.5580 mL | 1.1160 mL | 2.7901 mL | |
| 30 mM | 0.0930 mL | 0.4650 mL | 0.9300 mL | 2.3251 mL | |
| 40 mM | 0.0698 mL | 0.3488 mL | 0.6975 mL | 1.7438 mL | |
| 50 mM | 0.0558 mL | 0.2790 mL | 0.5580 mL | 1.3951 mL | |
| 60 mM | 0.0465 mL | 0.2325 mL | 0.4650 mL | 1.1625 mL | |
| 80 mM | 0.0349 mL | 0.1744 mL | 0.3488 mL | 0.8719 mL | |
| 100 mM | 0.0279 mL | 0.1395 mL | 0.2790 mL | 0.6975 mL |
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