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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Angiogenesis >Bcr-Abl inhibitors >WP1130

WP1130

WP1130 Structure
  • ₹0
  • Product name: WP1130
  • CAS: 856243-80-6
  • MF: C19H18BrN3O
  • MW: 384.27
  • EINECS:604-604-1
  • MDL Number:MFCD18839228
  • Synonyms:WP1130;(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylbutyl]-2-propenamide;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%
Manufacturer Product number Product description Packaging Price Updated Buy

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.

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning GHS hazard pictograms
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Description

Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype. WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37. At 5 μM, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells. Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.

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