BET BD2-IN-1
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research.
For research use only. We do not sell to patients.
- CAS No.: 2677039-24-4
- Formula: C30H30N4O2
- Molecular Weight:478.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD2 BD1 570 nM (IC50) |
BRD2 BD2 5.9 nM (IC50) |
BRD3 BD1 465 nM (IC50) |
BRD3 BD2 6.0 mM (IC50) |
BRD4 BD1 524 nM (IC50) |
BRD4 BD2 1.6 nM (IC50) |
BRDT BD1 527 nM (IC50) |
BET BD2-IN-1 (500 nM) effectively inhibits Th17 cell differentiation and has excellent selectivity for BD2 over BD1[1].
BET BD2-IN-1 (4 nM) binds to BRD4 BD2 in intact cells and has stabilization effect on BRD4 BD2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Th17 cells
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Concentration:500 nM
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Incubation Time:
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Result:Showed the strongest inhibitory activity and reduced differentiation from 19.0 to 7.81%.
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Cell Line:HEK 293 T cells
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Concentration:4, 20, 100, 500, 2500, 10000 nM
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Incubation Time:30 min
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Result:Stabilized BRD4 BD2 at 50.4 °C.
BET BD2-IN-1 (20 mg/kg for i.v; once daily for seven days) significantly decreases the disease activity index (DAI) score in dextran sulfate sodium (DSS) induced IBD mouse model[1].
Pharmacokinetic Analysis of BET BD2-IN-1 in Sprague Dawley Rats Model[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Imiquimod (HY-B0180)-induced Psoriasis mouse model[1]
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Dosage:10 and 20 mg/kg
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Administration:Intravenous injection (i.v.) ; Once daily for seven days
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Result:Significantly alleviated the Imiquimod-induced skin lesions in a dose-dependent manner.
Obviously reduced the enlarged spleen.
Significantly decreased the expression of p-STAT3 and p-NF-κB in mouse skin tissues.
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Animal Model:DSS (HY-116282C)-induced IBD mouse model[1]
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Dosage:10 and 20 mg/kg
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Administration:Intravenous injection (i.v.) ; Once daily for seven days
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Result:Effectively prevented colon shortening.
Effectively alleviated the DSS-induced weight loss.
Significantly alleviated the infiltration of inflammatory cells, areas of ulceration as well as loss of mucosal epithelium, and goblet cells caused by DSS.
Chemical Information
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CAS No. 2677039-24-4
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Molecular Weight 478.58
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Formula C30H30N4O2
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SMILES
O=C(C1=CC=CC(CN2C3=C(C=C4C5=C2C=CC=C5C(N4C)=O)C=CC=C3)=C1)NC6CCN(CC6)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BET BD2-IN-1 Related Classifications
HY-155680 Related Classifications
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