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- 產(chǎn)品描述: b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
- 靶點(diǎn): UCHL5/Usp14
- 體內(nèi)研究: b-AP15 (2.5 mg/kg) inhibits tumor growth in syngenic mice models with less frequent administration schedules. We administered b-AP15 to C57BL/6J mice with Lewis lung carcinomas (LLCs) using a 2-d-on, 2-d-off schedule and to BALB/c mice with orthotopic breast carcinoma (4T1) using a 1-d-on, 3-d-off schedule. b-AP15 significantly inhibited tumor growth in both models, with T/C=0.16 (P≤0.01) for the C57BL/6J mice and T/C=0.25 (P≤0.001) for the BALB/c mice. A reduction in the number of pulmonary metastases also is observed in the group of mice with 4T1 breast carcinomas treated with b-AP15
- 參考文獻(xiàn):
1. D'Arcy P, et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nat Med. 2011 Nov 6;17(12):1636-40. 2. Wang X, et al. The 19S Deubiquitinase Inhibitor b-AP15 is Enriched in Cells and Elicits Rapid Commitment to Cell Death. Mol Pharmacol. 2014 Jun;85(6):932-45. 3. Tian Z, et al. A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance. Blood. 2014 Jan 30;123(5):706-16.
- 溶解度: DMSO : 20 mg/mL (47.69 mM; Need ultrasonic)
- 保存條件: 2-8℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.384 ml 11.922 ml 23.844 ml 5 mM 0.477 ml 2.384 ml 4.769 ml 10 mM 0.238 ml 1.192 ml 2.384 ml 50 mM 0.048 ml 0.238 ml 0.477 ml
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