2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. Cbl-b-IN-16

Cbl-b-IN-16 (compound 31) 是口服有效的环指 E3 连接酶 Cbl-b 抑制剂，IC50 为 30 nM。 Cbl-b-IN-16 可以促进人 T 细胞中 IL-2 的产生，EC50 为 230 nM。Cbl-b-IN-16 具有抗肿瘤活性。

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Cbl-b-IN-16 Chemical Structure

Cbl-b-IN-16 Chemical Structure

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Cbl-b-IN-16 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

Cbl-b-IN-16 (compound 31) is an orally active Cbl-b inhibtor with IC50 of 30 nM and induces IL-2 production in Hu-T-cells with EC50 of 230 nM. Cbl-b-IN-16 exhibits antitumor activity[1].

IC50 & Target

IC50: Cbl-b (30 nM)[1]
体外研究
(In Vitro)

Cbl-b-IN-16 通过抑制 Cbl-b 泛素化和泛素到 Zap-70 的转移调节 TCR 信号通路，IC50 值分别是 63 nM 和 84 nM[1]。
Cbl-b-IN-16 (5 μM，20 min) 通过 SYK 抑制 Cbl-b 磷酸化[1]。
Cbl-b-IN-16 通过抑制作用增强 TCR 信号通路，从而上调 pPLCγ1 在人 T 细胞中的水平，EC50 为 0.61 μM[1]。

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

Cbl-b-IN-16 相关抗体:
体内研究
(In Vivo)

Cbl-b-IN-16 在 CD1 鼠和 Wistar Han 鼠体内的药代动力学特征如下表所示[1]：

Cbl-b-IN-16 在 CD1 鼠和 Wistar Han 鼠体内的药代动力学特征[1]

species route Dose (mg/kg) CL (mL/min/kg) Vss (L/kg) T1/2 (h) Cmax (μg/mL) Tmax (h) AUCinf (μg·h/mL) F (%) Calculated EHc
mouse iv 0.5 100 1.3 0.3 - - - - 0.66
mouse po 1.0 - - - 0.035 0.083 0.030 19 -
rat iv 0.5 55 1.6 0.45 - - - - 0.76
rat po 1.0 - - - 0.021 0.75 0.046 15 -

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

496.53

Formula

C26H27F3N6O
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

Cbl-b-IN-16 相关分类

  • 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)

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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)
× = ×
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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:

Cbl-b-IN-16E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseCbl-bubiquitinationIL-2T-cellsZap-70TCR-signalingPLCγInhibitorinhibitorinhibit

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目录号：
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