2. Cell Cycle/DNA Damage Apoptosis Autophagy
  3. p97 Caspase p62
  4. VCP/p97 IN-3

VCP/p97 IN-3 是一种 VCP/p97 变构抑制剂。 VCP/p97 IN-3 对 VCP 显示出抑制活性，IC50 为 9 nM，对突变型 VCP 蛋白的 IC50 分别为 12 nM (N660K) 和 19 nM (V474A/D649A)。VCP/p97 IN-3 增加 K48 泛素化水平和 caspase-3 的含量。VCP/p97 IN-3 激活内质网应激和未折叠蛋白反应 (UPR)。VCP/p97 IN-3 在 RPMI-8226 细胞皮下异种移植小鼠模型中抑制肿瘤生长。VCP/p97 IN-3 可用于多发性骨髓瘤的研究。

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VCP/p97 IN-3

VCP/p97 IN-3 Chemical Structure

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VCP/p97 IN-3 相关抗体

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma[1].

体内研究
(In Vivo)

VCP/p97 IN-3 (Compound 38) (50-100 mg/kg，腹腔注射，两天一次，持续 23 天) 在 RPMI-8226 细胞皮下异种移植小鼠模型中抑制肿瘤生长[1]。

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

Animal Model: RPMI-8226 cell subcutaneous xenograft mice[1]
Dosage: 50, 100 mg/kg
Administration: i.p. every other day, 23 days
Result: Increased the ubiquitin of K48 and the level of cleaved caspase-3.
Activated endoplasmic reticulum (ER)-stress and the UPR, as assessed by increases in phosphorylated-eIF2α (p-eIF2α), activation transcription factor 4 (ATF4),74 and glucose-regulated protein (BiP/GRP78).
Activated the DNA damage response as observed from the 2.5-fold increase in phosphorylated Histone 2A (H2A.X).
Reduced p62 levels.
Showed a TGI of 73% on day 23.
Suffered a mean 10% loss in body weight.
分子量

606.69

Formula

C31H32F2N6O3S
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

VCP/p97 IN-3 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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:

VCP/p97 IN-3p97Caspasep62VCPCdc48Sequestosome-1SQSTM1RPMI-8226 cellsVCP/p97multiple myelomacaspase-3ER-stressInhibitorinhibitorinhibit

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