WP1130
WP1130 Basic information
- Product Name:
- WP1130
- Synonyms:
-
- WP1130
- (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide
- WP1130;WP 1130;WP-1130
- CS-701
- DEGRASYN; WP 1130; WP-1130
- Degrasyn
- Degrasyn (WP1130)
- WP1130 ( Degrasyn )
- CAS:
- 856243-80-6
- MF:
- C19H18BrN3O
- MW:
- 384.27
- EINECS:
- 604-604-1
- Product Categories:
-
- Inhibitor
- Inhibitors
- Mol File:
- 856243-80-6.mol
WP1130 Chemical Properties
- Density
- 1.358
- storage temp.
- -20°
- solubility
- Soluble in DMSO (up to 45 mg/ml), or in Ethanol (up to 25 mg/ml).
- form
- solid
- color
- Yellow
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
WP1130 Usage And Synthesis
Description
WP1130 (856243-80-6) is a novel DUB inhibitor directly inhibiting USP9x, USP5, USP14 and UCH37 inducing rapid accumulation of polyubiquitinated proteins. Triggers tumor cell apoptosis.1 Blocks Jak2 signaling via Jak2 ubiquitination.2 WP-1130 causes ablation of the oncogenic transcription factor ERG in prostate cancer cells.3 See methyl analog WP1066.
Uses
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide can be used in biological study of drug screening and proteomic and metabolomic profiling to identify drug action mechanisms of breast cancer impaired pathogenicity.
in vivo
Degrasyn suppresses the growth of K562 heterotransplanted tumors as well as both wild-type Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3 cells transplanted into nude mice. To assess the possible therapeutic activity of Degrasyn against CML, nude mice received a subcutaneous transplant with K562 cells and are treated with 30 mg/kg Degrasyn every other day for 9 days after palpable tumor formation (10 days). This dose and schedule are well tolerated and effective in other tumor models. Antitumor activity is compared with that after daily Imatinib mesylate treatment (50 mg/kg). Nineteen days after tumor inoculation, tumors in the control group reached maximum allowable dimension, and the effect of therapy is assessed. Degrasyn treatment suppresses K562 tumor growth to an extent comparable to that observed in imatinib mesylate-treated animals, suggesting that Degrasyn is active in reducing the growth of established K562 tumors[1].
target
DUB
References
[1] VAIBHAV KAPURIA. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis.[J]. Cancer research, 2010, 70 22: 9265-9276. DOI:10.1158/0008-5472.can-10-1530
[2] VAIBHAV KAPURIA . A novel small molecule deubiquitinase inhibitor blocks Jak2 signaling through Jak2 ubiquitination[J]. Cellular signalling, 2011, 23 12: Pages 2076-2085. DOI:10.1016/j.cellsig.2011.08.002
[3] SHAN WANG. Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014: 4251-4256. DOI:10.1073/pnas.1322198111
WP1130Supplier
- Tel
- sales@boylechem.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- 0531-88811783
- sales@trio-pharmatech.com
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
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