产品描述: | VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM. |
靶点: |
IC50: appr 10 μM (Deubiquitinase);DUB |
体内研究: |
VLX1570 (3 mg/kg) significantly decreases tumor growth in mice bearing KMS-11 multiple myeloma cells. VLX1570 (4.4 mg/kg, i.p.) markedly suppresses tumor growth, without obvious weight loss and other signs of systemic toxicity in the Waldenstrom macroglobulinemia (WM)-bearing mice |
参考文献: |
1. Wang X, et al. Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15. Chem Biol Drug Des. 2015 Nov;86(5):1036-48. 2. Wang X, et al. The proteasome deubiquitinase inhibitor VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells. Sci Rep. 2016 Jun 6;6:26979. 3. Paulus A, et al. Coinhibition of the deubiquitinating enzymes, USP14 and UCHL5, with VLX1570 is lethal to ibrutinib- or bortezomib-resistant Waldenstrom macroglobulinemia tumor cells. Blood Cancer J. 2016 Nov 4;6(11):e492. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.13 ml |
10.652 ml |
21.304 ml |
5 mM |
0.426 ml |
2.13 ml |
4.261 ml |
10 mM |
0.213 ml |
1.065 ml |
2.13 ml |
50 mM |
0.043 ml |
0.213 ml |
0.426 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |