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WP1130

Product Name
WP1130
CAS No.
856243-80-6
Chemical Name
WP1130
Synonyms
WP1130;CS-701;Degrasyn;Degrasyn, >=98%;WP1130 USP/EP/BP;Degrasyn (WP1130);WP1130 ( Degrasyn );WP1130;WP 1130;WP-1130;Degrasyn, 10 mM in DMSO;Degrasyn (WP1130) ，S2243
CBNumber
CB82561501
Molecular Formula
C19H18BrN3O
Formula Weight
384.27
MOL File
856243-80-6.mol
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WP1130 Property

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.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
681685
Product name
WP1130
Purity
A cell-permeable tyrphostin compound that acts as a partially selective deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway.
Packaging
10MG
Price
$172
Updated
2025/07/31
Cayman Chemical
Product number
15227
Product name
WP1130
Purity
≥95%
Packaging
5mg
Price
$68
Updated
2024/03/01
Cayman Chemical
Product number
15227
Product name
WP1130
Purity
≥95%
Packaging
10mg
Price
$121
Updated
2024/03/01
Cayman Chemical
Product number
15227
Product name
WP1130
Purity
≥95%
Packaging
25mg
Price
$286
Updated
2024/03/01
Cayman Chemical
Product number
15227
Product name
WP1130
Purity
≥95%
Packaging
50mg
Price
$535
Updated
2024/03/01
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WP1130 Chemical Properties,Usage,Production

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

WP1130 Preparation Products And Raw materials

Raw materials

Preparation Products

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WP1130 Suppliers

Canada 1 China 106 India 1 United Kingdom 1 United States 17 Global 126
Dalton Chemical Laboratories, Inc.
Tel
--
Fax
--
Email
chemist@dalton.com
Country
Canada
ProdList
965
Advantage
78

856243-80-6, WP1130Related Search:

17-AAG TCPOBOP Vorinostat CYCLOPAMINE 3--Phenyl-N-(2,2,2-trichloro-1-((((4-chlorophenyl)amino)carbonothioyl)amino)ethyl)acrylamide WP1066 (2E)-3-(4'-Hydroxy-3'-tricyclo[3.3.1.13,7]dec-1-yl[1,1'-biphenyl]-4-yl)-2-propenoic acid Pracinostat BAY 11-7085 ML264 Bortezomib PR-619 MK-2206 2HCl Sunitinib Malate P-5091 PLX4032

  • 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 )
  • (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide
  • (2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide Degrasyn (WP1130)
  • Degrasyn, >=98%
  • 2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-, (2E)-
  • WP1130 USP/EP/BP
  • Degrasyn, 10 mM in DMSO
  • Degrasyn (WP1130) ，S2243
  • 856243-80-6
  • Inhibitor
  • Inhibitors