VLX1570
- Product Name
- VLX1570
- CAS No.
- 1431280-51-1
- Chemical Name
- VLX1570
- Synonyms
- CS-2226;VLX1570;VLX1570 (VLX 1570;1-Acryloyl-3,5-bis(4-fluoro-3-nitrobenzylidene)azepan-4-one;VLX1570,Inhibitor,Deubiquitinase,VLX-1570,DUBs,VLX 1570,inhibit;1-acryloyl-3,5-bis((E)-4-fluoro-3-nitrobenzylidene)azepan-4-one;(3Z,5Z)-1-Acryloyl-3,5-bis(4-fluoro-3-nitrobenzylidene)azepan-4-one;(3E,5E)-1-Acryloyl-3,5-bis(4-fluoro-3-nitrobenzylidene)hexahydro-4H-azepin-4-one;4H-Azepin-4-one, 3,5-bis[(4-fluoro-3-nitrophenyl)methylene]hexahydro-1-(1-oxo-2-propen-1-yl)-
- CBNumber
- CB63133354
- Molecular Formula
- C23H17F2N3O6
- Formula Weight
- 469.39
- MOL File
- 1431280-51-1.mol
VLX1570 Property
- 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
N-Bromosuccinimide Price
- Product number
- 29721
- Product name
- VLX1570
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
- Product number
- 29721
- Product name
- VLX1570
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $223
- Updated
- 2024/03/01
- Product number
- 29721
- Product name
- VLX1570
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $469
- Updated
- 2024/03/01
- Product number
- 29721
- Product name
- VLX1570
- Packaging
- 500μg
- Price
- $35
- Updated
- 2021/12/16
- Product number
- 29721
- Product name
- VLX1570
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
VLX1570 Chemical Properties,Usage,Production
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.