WP1130
(Synonyms: WP 1130; WP-1130) 目录号 : GC10970A deubiquitinase inhibitor
Cas No.:856243-80-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
WP1130, also known as degrasyn, is a second-generation tyrphostin derivative initially identified as a Janus-activated kinase (JAK)-signal transducer and activator of transcription (STAT) pathway inhibitor that reduces STAT activation stimulated by cytokines (such as IL-6 and IL-3) through the rapid down-regulation of upstream JAK kinases. WP1130 has also been identified as a selective deubiquitinating enzyme (DUB) inhibitor that directly inhibits DUB activity of USP9x, USP5, USP14 and UCH37 leading to rapid accumulation of polyubiquitinated proteins into juxtanuclear aggresomes and tumor cell apoptosis. WP1130-induced apoptosis and anti-proliferation in tumor cells have been implicated in the treatment of chronic myelogenous leukemia (CML), melanoma, glioblastoma and myeloproliferative disorders.
References:
[1]Kapuria V1, Peterson LF, Fang D, Bornmann WG, Talpaz M, Donato NJ. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Res. 2010 Nov 15;70(22):9265-76. doi: 10.1158/0008-5472.CAN-10-1530. Epub 2010 Nov 2.
[2]Bartholomeusz GA1, Talpaz M, Kapuria V, Kong LY, Wang S, Estrov Z, Priebe W, Wu J, Donato NJ. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood. 2007 Apr 15;109(8):3470-8. Epub 2007 Jan 3.
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6023 mL | 13.0117 mL | 26.0234 mL |
5 mM | 0.5205 mL | 2.6023 mL | 5.2047 mL |
10 mM | 0.2602 mL | 1.3012 mL | 2.6023 mL |
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