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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-VLX1570
VLX1570

Chemical Structure : VLX1570

CAS No.: 1431280-51-1

VLX1570 (VLX 1570;VLX-1570)

货号: PC-43050Not For Human Use, Lab Use Only.

VLX1570 is a small molecule b-AP15 analog that fucttion as proteasome deubiquitinase inhibitor with IC50 of 10 uM, interacts at the active sites of the proteasome DUBs USP14 and UCHL5.

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10 mg ¥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VLX1570 is a small molecule b-AP15 analog that fucttion as proteasome deubiquitinase inhibitor with IC50 of 10 uM, interacts at the active sites of the proteasome DUBs USP14 and UCHL5.
VLX1570 demonstrates cytotoxicity in survival assays in HCT116 colon cancer cells with IC50 of 0.58 uM, shows no inhibitory activity on a panel of recombinant non-proteasome DUBs, recombinant kinases, or caspase-3.
VLX1570 decreases cell viability in chemotherapy resistant endometrial cancer cells consistent with cell cycle arrest and caspase-3 mediated apoptosis.
VLX1570 decreases tumor burden and prolongs survival in WM-xenografted mice.

物理化学性质&存储条件

分子量 469.3944
分子式 C23H17F2N3O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

4H-Azepin-4-one, 3,5-bis[(4-fluoro-3-nitrophenyl)methylene]hexahydro-1-(1-oxo-2-propen-1-yl)-

参考文献

1. Wang X, et al. Chem Biol Drug Des. 2015 Nov;86(5):1036-48.

2. Vogel RI, et al. Oncotarget. 2016 May 24;7(21):30962-76.

3. Shukla N, et al. Cancer Res. 2016 Aug 1;76(15):4525-34.

4. Wang X, et al. Sci Rep. 2016 Jun 6;6:26979. doi: 10.1038/srep26979.

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