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VLX1570

VLX1570 Struktur
1431280-51-1
CAS-Nr.
1431280-51-1
Englisch Name:
VLX1570
Synonyma:
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
Summenformel:
C23H17F2N3O6
Molgewicht:
469.39
MOL-Datei:
1431280-51-1.mol

VLX1570 Eigenschaften

storage temp. 
Store at -20°C
L?slichkeit
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)
Aggregatzustand
A crystalline solid
Farbe
Light yellow to yellow

Sicherheit

VLX1570 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

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.

Verwenden

VLX1570 is a proteasome deubiquitinase inhibitor. It also exhibits antineoplastic activities.

VLX1570 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


VLX1570 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 67)Lieferanten
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ATK CHEMICAL COMPANY LIMITED
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TargetMol Chemicals Inc.

support@targetmol.com United States 38469 58
Hebei Miaoyin Technology Co.,Ltd
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kathy@hbyinsheng.com China 3512 58
Aceschem Inc.
+1-817863-6948 +1-(817)863-6948
sales@aceschem.com United States 19632 58

  • 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
  • 1-acryloyl-3,5-bis((E)-4-fluoro-3-nitrobenzylidene)azepan-4-one
  • 1431280-51-1
  • C23H17F2N3O6
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