2. Epigenetics
  3. Epigenetic Reader Domain
  4. BET BD2-IN-1

BET BD2-IN-1 (compound 45) 是一种有效的 BET BD2 选择性抑制剂 (IC50 为1.6 nM)。它通过降低 STAT3 和 NF-κB 的活性来抑制 Th17 细胞的分化。 BET BD2-IN-1 可用于研究银屑病和炎症性肠病。

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BET BD2-IN-1 Chemical Structure

BET BD2-IN-1 Chemical Structure

CAS No. : 2677039-24-4

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BET BD2-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

BET BD2-IN-1 (500 nM) 能有效抑制 Th17 细胞分化，对 BD2 的选择性优于 BD1[1]。
BET BD2-IN-1 (4 nM) 在完整细胞中与 BRD4 BD2 结合，对 BRD4 BD2 具有稳定效应[1]。

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

BET BD2-IN-1 相关抗体:

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.
体内研究
(In Vivo)

BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 可抑制小鼠皮肤组织中 p-STAT3 和 p-NF-κB 蛋白的表达，有效改善银屑病小鼠模型的病理改变[1]。
BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 显著降低 DSS 诱导的 IBD 小鼠模型疾病活动指数 (DAI) 评分[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

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

Formula

C30H30N4O2

CAS 号

2677039-24-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
产品使用指南 (1538 KB)
参考文献

BET BD2-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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目录号：
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