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  3. I-BET282E

I-BET282E 是八种 BET bromodomains 泛抑制剂,对其他代表性含溴代烷的蛋白质具有选择性。I-BET282E 对 8 种 BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), BRD4 (BD1/BD) 的 pIC50 值为 6.4-7.7。

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I-BET282E Chemical Structure

I-BET282E Chemical Structure

CAS No. : 2885162-99-0

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I-BET282E 的其他形式现货产品:

Customer Review

Other Forms of I-BET282E:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD)[1].

体外研究
(In Vitro)

I-BET282E has a weak inhibition of the hERG potassium ion channel (pIC50 4.4-5.1 in a variety of assay formats). I-BET282E shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4[1].

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

体内研究
(In Vivo)

I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively[1].
I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively[1].

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

分子量

546.64

Formula

C26H34N4O7S

CAS 号
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
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  • 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.

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产品名称:
I-BET282E
目录号:
HY-19760B
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