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 is an allosteric p97 inhibitor with an IC 50 of approximately 27 nM. UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC 50 =300 nM) and shows 3-fold resistance for p97 mutant T688A. UPCDC-30245 can be used in the research of cancer.

Solid

allosteric p97 27 nM (IC50) wild type p97

UPCDC-30245 binds at the junction between the D1 dan D2 domains of p97.
UPCDC-30245 inhibits cell proliferation in HeLa, A549, BxPC-3, PRMI8226, MM1S, HCT116 cells, and appears more potent in HT29 cells.
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).
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Banerjee S, et al. 2.3 ? 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.

In Vitro: DMSO : 250 mg/mL (539.22 mM; Need ultrasonic)配制储备液