1. PROTAC
  2. PROTACs
  3. ZXH-4-130

ZXH-4-130 是一种高效、选择性的 CRBN 降解剂。ZXH-4-130 是一种 CRBN-VHL 化合物 (hetero-PROTAC)。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 ZXH-4-130 TFA 通常具有更好的水溶性和稳定性。

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ZXH-4-130 Chemical Structure

ZXH-4-130 Chemical Structure

CAS No. : 2711006-66-3

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ZXH-4-130 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZXH-4-130 is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC)[1].

IC50 & Target[1]

VHL

 

体外研究
(In Vitro)

ZXH-4-130 (100 nM; 2 h pre-treatments; followed by 96-hour treatment with 1 μM of Pomalidomide) prevents Pomalidomide (1 μM) cytotoxicity to a significant extent, ZXH-4-130 has statistically significant amounts of prevention[1].
MM1.S cells are pre-treated for 2 h with 50 nM of ZXH-4-130, before exposing them to CC-885, a compound that induces G1 to S phase transition protein 1 (GSPT1) degradation via CRBN E3 ligase recruitment. Pretreatment with 50 nM of ZXH-4-130 rescues GSPT1 degradation[1].
ZXH-4-130 (100 nM 2 h pre-treatment; followed by 6 h treatment with THAL-SNS-032) induces nearly complete CRBN degradation, but THAL-SNS-032's activity against CDK9 is only partially prevented[1].

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

Cell Viability Assay[1]

Cell Line: MM1.S cells
Concentration: 100 nM
Incubation Time: 2 h pre-treatments; followed by 96-hour treatment with 1 μM of Pomalidomide
Result: Prevented Pomalidomide cytotoxicity to a significant extent, ZXH-4-130 has statistically significant amounts of prevention.

Western Blot Analysis[1]

Cell Line: MM1.S cells
Concentration: 50 nM
Incubation Time: 2 h pretreatment with ZXH-4-130, followed by 4 h treatment with CC-885
Result: Rescued GSPT1 degradation.
分子量

871.05

Formula

C46H58N6O9S

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

ZXH-4-130 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)

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:
ZXH-4-130
目录号:
HY-132857
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