| 產(chǎn)品描述： | b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14. |
| 靶點(diǎn)： |
UCHL5/Usp14;Apoptosis;DUB |
| 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. |
| 溶解性： |
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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