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Submit ReviewAZ1 USP25/28 inhibitor is a selective inhibitor of USP28 (IC50 = 0.6 μM, Kd= 0.2 - 3.7 μM) and USP25 (IC50 = 0.7 μM). AZ1 USP25/28 inhibitor exhibits selectivity for USP25 and USP28 over other DUB family members. The compound dose-dependently reduces c-Myc levels in colon carcinoma cells in vitro and induces cell death (EC50 values are 18 - 20 μM). In a mouse Alzheimer's disease model, AZ1 USP25/28 inhibitor reduces amyloid burden, attenuates microglial activation and improves synaptic and cognitive function.
分子量 | 422.21 |
公式 | C17H16BrF4NO2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2165322-94-9 |
PubChem ID | 135397656 |
InChI Key | ITHSFXDGKQYOED-UHFFFAOYSA-N |
Smiles | FC1=CC=C(COC2=CC=C(C=C2CNCCO)Br)C=C1C(F)(F)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 42.22 | 100 |
以下数据基于产品分子量 422.21。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.37 mL | 11.84 mL | 23.68 mL |
5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
10 mM | 0.24 mL | 1.18 mL | 2.37 mL |
50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
Wrigley et al (2017) Identification and characterization of dual inhibitors of the USP25/28 deubiquitinating enzyme subfamily. ACS Chem.Biol. 12 3113 PMID: 29131570
Zheng et al (2021) Trisomy 21-induced dysregulation of microglial homeostasis in Alzheimer's brains is mediated by USP25. Sci.Adv. 7 eabe1340 PMID: 33523861
Zheng et al (2022) USP25 inhibition ameliorates Alzheimer's pathology through the regulation of APP processing and Aβ generation. J.Clin.Invest. 132 e152170 PMID: 35229730
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关键词: AZ1 USP25/28 inhibitor, AZ1 USP25/28 inhibitor supplier, USP25, USP28, inhibitors, inhibits, selective, deubiquitinating, enzymes, c-Myc, Alzheimer's, disease, amyloid, neuroinflammation, Deubiquitinating, Enzymes, 7845, Tocris Bioscience
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