UPCDC-30245

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

UPCDC-30245 

UPCDC-30245 是一种变构 p97 (allosteric p97) 抑制剂，IC50 约为 27 nM。UPCDC-30245 抑制 p97 突变体 N660K 的效力与野生型 (IC50=300 nM) 相似，此外对 p97 突变体 T688A 仅表现出 3 倍的耐药性。UPCDC-30245可用于癌症研究。

UPCDC-30245

UPCDC-30245 Chemical Structure

CAS No. : 1883351-01-6

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生物活性

UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM[1]. UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A[2]. UPCDC-30245 can be used in the research of cancer[1][2][3].

IC50 & Target[1][2]

allosteric p97

27 nM (IC50)

wild type p97

300 nM (IC50)

体外研究
(In Vitro)

UPCDC-30245 binds at the junction between the D1 dan D2 domains of p97[1].
UPCDC-30245 inhibits cell proliferation in HeLa, A549, BxPC-3, PRMI8226, MM1S, HCT116 cells, and appears more potent in HT29 cells[2].
UPCDC-30245 (0.01-100 μM) shows anti-proliferative effects on parental and CB-5083 resistant HCT116 cell lines that harbor a new p97 double mutation (D649A/T688A)[2].
UPCDC-30245 (4 μm; 2, 6, 10, 18, 24 hours; functional enrichment analysis) is not linked to pathways typically impacted by p97 inhibition, such as protein processing in the ER, UPR, and asparagine N-linked glycosylation[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

463.63

Formula

C28H38FN5
CAS 号

1883351-01-6
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]. Banerjee S, et al. 2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition. Science. 2016 Feb 19;351(6275):871-5.

    [2]. Wang F, et al. Allosteric p97 Inhibitors Can Overcome Resistance to ATP-Competitive p97 Inhibitors for Potential Anticancer Therapy. ChemMedChem. 2020 Apr 20;15(8):685-694.

    [3]. Wang F, et al. Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition. Cell Chem Biol. 2021 Nov 23:S2451-9456(21)00482-7.

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