VCP/p97 inhibitor-1

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VCP/p97 inhibitor-1 

VCP/p97 inhibitor-1 是一种有效的 VCP/p97 (也称为 Cdc48，CDC-. 48，或 Ter94) 抑制剂，IC50 值为 54.7 nM。VCP/p97 inhibitor-1 导致蛋白质稳态失调并干扰泛素-蛋白酶体系统 (UPS) 对错误折叠多肽的降解。

VCP/p97 inhibitor-1

VCP/p97 inhibitor-1 Chemical Structure

CAS No. : 2630950-38-6

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生物活性

VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS)[1][2].

IC50 & Target

54.7 nM (VCP/p97)[1]
体外研究
(In Vitro)

VCP/p97 inhibitor-1 (compound 17) (3-fold serial dilutions with the highest concentration at 10 μM; 72 hours) has anti-proliferation effect with IC50s of 2.9 and 0.86 μM in A549 and RPMI8226 cells, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549, RPMI8226 cells
Concentration: 3-fold serial dilutions with the highest concentration at 10 μM
Incubation Time: 72 hours
Result: Showed anti-proliferative rates in A549 and RPMI8226 cells (IC50= 2.9 and 0.86 μM, respectively).

分子量

491.37

Formula

C24H26BN5O4S
CAS 号

2630950-38-6
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.
参考文献

  • [1]. Zhang Y, et al. Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors. Bioorg Med Chem. 2021;38:116114.

    [2]. van den Boom J, et al. VCP/p97-Mediated Unfolding as a Principle in Protein Homeostasis and Signaling. Mol Cell. 2018;69(2):182-194.

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