2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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.

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BET BD2-IN-1

BET BD2-IN-1 構造式

CAS 番号 : 2677039-24-4

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BET BD2-IN-1 関連抗体

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製品説明

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[1].

IC50 & Target

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)

体外実験

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.

BET BD2-IN-1 関連抗体

Cell Differentiation Assay[1]

Cell Line: Th17 cells
Concentration: 500 nM
Incubation Time:
Result: Showed the strongest inhibitory activity and reduced differentiation from 19.0 to 7.81%.

Cell Migration Assay [1]

Cell Line: HEK 293 T cells
Concentration: 4, 20, 100, 500, 2500, 10000 nM
Incubation Time: 30 min
Result: Stabilized BRD4 BD2 at 50.4 °C.
体内実験

BET BD2-IN-1 (20 mg/kg for i.v; once daily for seven days) inhibits the protein expression of p-STAT3 and p-NF-κB in mouse skin tissues, effectively ameliorates the pathological changes in the psoriasis mouse model[1].
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]

parameter AUC(0‑t) (ng•h/mL) C0 (ng/mL) T1/2 (h) CL (mL/kg/min) Vdss (L/kg)
iv(1 mg/kg) 272 ± 7.2 279 ± 78 1.5 ± 0.1 60 ± 2.0 6.6 ± 0.8
parameter AUC(0‑t) (ng•h/mL) Cmax (ng/mL) T1/2 (h) Tmax (h) F (%)
po(10 mg/kg) 78 ± 34 20 ± 11 1.9 ± 0.2 2.7 ± 1.2 2.9 ± 1.2

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Imiquimod (HY-B0180)-induced Psoriasis mouse model[1]
Dosage: 10 and 20 mg/kg
Administration: Intravenous injection (i.v.) ; Once daily for seven days
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.
Animal Model: DSS (HY-116282C)-induced IBD mouse model[1]
Dosage: 10 and 20 mg/kg
Administration: Intravenous injection (i.v.) ; Once daily for seven days
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.
分子量

478.58

分子式

C30H30N4O2

CAS 番号

2677039-24-4

SMILES

O=C(C1=CC=CC(CN2C3=C(C=C4C5=C2C=CC=C5C(N4C)=O)C=CC=C3)=C1)NC6CCN(CC6)C

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション
取扱説明書 (2659 KB)
参考文献
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BET BD2-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BET BD2-IN-12677039-24-4Epigenetic Reader DomainBET BD2PsoriasisInflammatory Bowel DiseaseIBDInhibitorinhibitorinhibit

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BET BD2-IN-1
製品番号:
HY-155680
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