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BET BD2-IN-1

Catalog No. T79527

BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation through the reduced activation of STAT3 and NF-κB, making it relevant in research on psoriasis and inflammatory bowel disease (IBD) [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BET BD2-IN-1, CAS N/A

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation through the reduced activation of STAT3 and NF-κB, making it relevant in research on psoriasis and inflammatory bowel disease (IBD) [1].
Targets&IC50	BRD2 BD1:570 nM, BRD2 BD2:5.9 nM, BRD3 BD1:465 nM, BRD3 BD2:6.0 mM, BRD4 BD1:524 nM, BRD4 BD2:1.6 nM, BRDT BD1:527 nM
In vitro	BET BD2-IN-1 at a concentration of 500 nM effectively inhibits Th17 cell differentiation, exhibiting greater selectivity for BD2 over BD1 [1]. Additionally, at 4 nM, BET BD2-IN-1 interacts with BRD4 BD2 in a whole-cell context, demonstrating a stable effect on BRD4 BD2 [1].
In vivo	BET BD2-IN-1 administered intravenously at 20 mg/kg once daily for seven consecutive days inhibited the expression of p-STAT3 and p-NF-κB proteins in the skin tissues of mice, effectively ameliorating pathological alterations in a psoriasis mouse model [1]. The same treatment regimen significantly reduced the Disease Activity Index (DAI) scores in a DSS-induced inflammatory bowel disease (IBD) mouse model [1]. The pharmacokinetic analysis of BET BD2-IN-1 in Sprague-Dawley rats indicated parameters including AUC(0‑t) (ng•h/mL), C0 (ng/mL), T1/2 (h), CL (mL/kg/min), and Vdss (L/kg) [1].

Molecular Weight

N/A

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BET BD2-IN-1 Chromatin/Epigenetic Epigenetic Reader Domain inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.