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Merck
CN

SML3584

Sigma-Aldrich

AZ1

≥98% (HPLC)

别名:

2-[[[5-Bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]-ethanol, AZ 1, AZ-1

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About This Item

经验公式(希尔记法):
C17H16BrF4NO2
分子量:
422.21
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.21

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).

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

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分析证书(COA)

Lot/Batch Number

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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)
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)
Inhibition of USP28 overcomes Cisplatin-resistance of squamous tumors by suppression of the Fanconi anemia pathway
Cell Death and Differentiation, 29, 568-584 (2022)
Deubiquitylase USP25 prevents degradation of BCR-ABL protein and ensures proliferation of Ph-positive leukemia cells
Oncogene, 39, 3867-3878 (2020)
The deubiquitinase USP25 supports colonic inflammation and bacterial infection and promotes colorectal cancer
Nature cancer, 1, 811-825 (2020)

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