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UPCDC-30245
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UPCDC-30245图片
CAS NO:1883351-01-6
包装:5mg
市场价:4050元

产品介绍
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。
Cas No.1883351-01-6
分子式C28H38FN5
分子量463.63
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

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].

[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.