- VLX1570
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- $97.00
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2026-07-27
- CAS:1431280-51-1
- Purity: 99.57%
- Supply Ability: 10g
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| | VLX1570 Basic information |
| Product Name: | VLX1570 | | Synonyms: | VLX1570;CS-2226;VLX1570 (VLX 1570;4H-Azepin-4-one, 3,5-bis[(4-fluoro-3-nitrophenyl)methylene]hexahydro-1-(1-oxo-2-propen-1-yl)-;(3Z,5Z)-1-Acryloyl-3,5-bis(4-fluoro-3-nitrobenzylidene)azepan-4-one;1-Acryloyl-3,5-bis(4-fluoro-3-nitrobenzylidene)azepan-4-one;VLX1570,Inhibitor,Deubiquitinase,VLX-1570,DUBs,VLX 1570,inhibit;(3E,5E)-1-Acryloyl-3,5-bis(4-fluoro-3-nitrobenzylidene)hexahydro-4H-azepin-4-one | | CAS: | 1431280-51-1 | | MF: | C23H17F2N3O6 | | MW: | 469.4 | | EINECS: | | | Product Categories: | | | Mol File: | 1431280-51-1.mol |  |
| | VLX1570 Chemical Properties |
| Boiling point | 722.324±60.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.457±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | storage temp. | Store at -20°C | | solubility | DMF:25.0(Max Conc. mg/mL);53.26(Max Conc. mM)
DMF:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.64(Max Conc. mM)
DMSO:47.0(Max Conc. mg/mL);100.13(Max Conc. mM) | | form | A crystalline solid | | pka | -1.237±0.20(predicted) | | color | Light yellow to yellow |
| | VLX1570 Usage And Synthesis |
| Description | VLX1570 is an inhibitor of 19S proteasomal deubiquitinases with IC50 values of 6.4 and 13 μM for deubiquitinase activity in vitro using Ub-rhodamine and Ub-AMC, respectively, as substrates. It is selective for proteasomal deubiquitinases over a panel of deubiquitinases at 20 μM, but inhibits USP5 by greater than 50%, and over a panel of 211 kinases at 10 μM, but inhibits Cdk4 by 77%. VLX1570 binds to and inhibits recombinant ubiquitin-specific protease 14 (USP14) and ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5) in vitro, and inhibits the USP14 and UCHL5 activity of purified 19S proteasomes when used at a concentration of 50 μM. It inhibits the proliferation of KMS-11, RPMI-8226, OPM-2, and OPM-2-BZR multiple myeloma cells (IC50s = 43, 74, 126, and 191 nM, respectively), as well as induces apoptosis and increases the accumulation of polyubiquitinated proteins. VLX1570 (3 mg/kg per day for 10 days) increases survival and reduces tumor growth in KMS-11-LUC2 and RPMI-8226 mouse xenograft models, respectively. | | Uses | VLX1570 is a proteasome deubiquitinase inhibitor. It also exhibits antineoplastic activities. | | in vivo | VLX1570 (3mg/kg) significantly decreases tumor growth in mice bearing KMS-11 multiple myeloma cells[2]. VLX1570 (4.4mg/kg, i.p.) markedly suppresses tumor growth, without obvious weight loss and other signs of systemic toxicity in the Waldenstrom macroglobulinemia (WM)-bearing mice[3]. | | References | [1] XIN WANG. Synthesis and Evaluation of Derivatives of the Proteasome Deubiquitinase Inhibitor b-AP15[J]. Chemical Biology & Drug Design, 2015, 86 5: 1036-1048. DOI: 10.1111/cbdd.12571
[2] XIN WANG. The proteasome deubiquitinase inhibitor VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells.[J]. Scientific Reports, 2016: 26979. DOI: 10.1038/srep26979
[3] CHIA-CHUAN CHO. Drug Repurposing for the SARS-CoV-2 Papain-Like Protease[J]. ChemMedChem, 2021, 17 1. DOI: 10.1002/cmdc.202100455 |
| | VLX1570 Preparation Products And Raw materials |
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