1. Epigenetics
  2. Epigenetic Reader Domain
  3. I-BET432

I-BET432 是一种 BET 抑制剂。I-BET432 抑制 BRD4 的 N 端溴化域 (BD1) 和 C 端溴化域 (BD2) 的 pIC50 值分别为 7.5 和 7.2。I-BET432 可作为多种肿瘤和炎症疾病研究的口服候选分子。

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I-BET432 Chemical Structure

I-BET432 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases[1].

体外研究
(In Vitro)

I-BET432 inhibits BRD4 BD1 and BD2 with pIC50 values of 7.5 and 7.2, respectively[1].
I-BET432 inhibits human whole blood MCP-1 with an pIC50 value of 7.4[1].
I-BET432 inhibits hERG with an pIC50 value <4.3[1].

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

体内研究
(In Vivo)

I-BET432 shows great oral bioavailability in rats and dogs[1].
1.19 Pharmacokinetic Properties of I-BET432 in Rats and Dogs[1].

Rats
PO/IV 3/1 mg/kg
Dogs
PO/IV 1.5/0.5 mg/kg
CLb (mL/min/kg) 26 28
CLb,u (mL/min/kg) 38 20
Vss (L/kg) 1.3 2.7
Vss,u (L/kg) 1.9 5.7
t1/2 (h) 0.74 1.4
Fpo (%) 67 79
fub 0.68 0.47

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

分子量

327.38

Formula

C18H21N3O3

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
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
I-BET432
目录号:
HY-151894
需求量: