推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
FC1=CC=C(COC2=CC=C(C=C2CNCCO)Br)C=C1C(F)(F)F
InChI key
ITHSFXDGKQYOED-UHFFFAOYSA-N
生化/生理作用
AZ1 is a potent and selective dual USP25 & USP28 deubiquitinase (DUBs) inhibitor (USP25/28 IC50 = 0.62/0.7 nM by Ub-Rh110 assay) that induces HCT116 cellular c-Myc degradation (20-100 µM for 3h or 60 µM for 0.3-3h). AZ1 exhibits antiproliferation activity in cancer cultures (IC50 ≤20 µM; HCT116, HT29 and SW480) and anti-tumor efficacy in an orthotopic model of lung SCC tumours in mice in vivo (125 mg/kg or 375 mg/kg i.p. once every three days, 6 injections total).
Potent and selective dual USP25 & USP28 deubiquitinase (DUBs) inhibitor with anti-cancer efficacy in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
The deubiquitinase USP25 supports colonic inflammation and bacterial infection and promotes colorectal cancer
Nature cancer, 1, 811-825 (2020)
Deubiquitylase USP25 prevents degradation of BCR-ABL protein and ensures proliferation of Ph-positive leukemia cells
Oncogene, 39, 3867-3878 (2020)
Inhibition of USP28 overcomes Cisplatin-resistance of squamous tumors by suppression of the Fanconi anemia pathway
Cell Death and Differentiation, 29, 568-584 (2022)
Maintaining protein stability of ?Np63 via USP28 is required by squamous cancer cells
Cristian Prieto-Garcia, Oliver Hartmann, Michaela Reissland, Fabian Braun, Thomas Fischer
EMBO Molecular Medicine, 12 (2022)
USP28 enables oncogenic transformation of respiratory cells, and its inhibition potentiates molecular therapy targeting mutant EGFR, BRAF and PI3K
Molecular Oncology, 16, 3082-3106 (2022)
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