An inhibitor of 19S proteasomal deubiquitinases (IC50s = 6.4 and 13 μM for deubiquitinase activity in vitro using Ub-rhodamine and Ub-AMC

VLX1570 – 5 mg

Brand:
Cayman
CAS:
1431280-51-1
Storage:
-20
UN-No:
Non-Hazardous - /

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.{53378,53379} 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%.{53378} 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.{53378,53379} 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.{53379} 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.  

 

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Description

An inhibitor of 19S proteasomal deubiquitinases (IC50s = 6.4 and 13 μM for deubiquitinase activity in vitro using Ub-rhodamine and Ub-AMC, respectively, as substrates); selective for proteasomal deubiquitinases over a panel of deubiquitinases at 20 μM, but inhibits USP5 by >50%, and over a panel of 211 kinases at 10 μM, but inhibits Cdk4 by 77%; binds to and inhibits recombinant USP14 and UCHL5 in vitro; inhibits the USP14 and UCHL5 activity of purified 19S proteasomes at 50 μM; 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; increases survival and reduces tumor growth in KMS-11-LUC2 and RPMI-8226 mouse xenograft models, respectively, at 3 mg/kg per day for 10 days

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

Synonyms: 

Molecular weight: 469.4

CAS: 1431280-51-1

Purity: ≥98%

Formulation: A crystalline solid

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