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925225

Sigma-Aldrich

KB02yne

Synonyme(s) :

2-Chloro-1-(6-(hex-5-yn-1-yloxy)-3,4-dihydroquinolin-1(2H)-yl)ethan-1-one, Functionalized scout fragment

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About This Item

Formule empirique (notation de Hill):
C17H20ClNO2
Numéro CAS:
2376152-06-4
Poids moléculaire :
305.80
Code UNSPSC :
12352101
Nomenclature NACRES :
NA.22

Forme

powder or crystals (or Solid or Liquid)

Niveau de qualité

100

Pertinence de la réaction

reagent type: chemical modification reagent
reaction type: click chemistry

Température de stockage

2-8°C

Catégories apparentées

Application

KB02yne is a cysteine-reactive small-molecule fragment for chemoproteomic and ligandability studies for both traditionally druggable proteins as well as ″undruggable,″ or difficult-to-target, proteins. This fragment electrophile is the functionalized version of KB02 (912131).

Related useful products may include:
  • Cysteine-reactive fragments: KB02 (912131), KB03 (912654), KB05 (911798), sulfoxide (925136), CoLDR probe (923818)
  • Functionalized scout fragments: KB02-COOH (925047), KB05yne (925144)
  • Electrophilc degraders featuring scout fragments: KB02-SLF (914738), KB03-SLF (914975), KB05-SLF (913715), Biotin-SLF (914223)
  • Cysteine-reactive probes for chemoproteomics: IA alkyne (924237), IA 5-TAMRA (925020), desthiobiotin iodoacetamide (923826), or biotin iodoacetamide (B2059)

Technology spotlight: Proteomic Ligandability Assessment

Autres remarques

Functionalized Scout Fragments for Site-Specific Covalent Ligand Discovery and Optimization

The Proteome-Wide Potential for Reversible Covalency at Cysteine

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

Produit(s) apparenté(s)

Réf. du produit
Description
Tarif

B2059

Biotin Polyethyleneoxide Iodoacetamide

699357

4-(Chloroacetyl)morpholine, 97%

911798

N-(4-Bromophenyl)-N-phenylacrylamide, ≥95%

912131

2-Chloro-1-(6-methoxy-1,2,3,4-tetrahydroquinolin-1-yl)ethan-1-one, ≥95%

912654

N-(3,5-Bis(trifluoromethyl)phenyl)-2-chloroacetamide, ≥95%

914975

KB03-SLF, ≥95%

913715

KB05-SLF

914738

KB02-SLF, ≥95%

914223

Biotin-SLF

923818

N-(But-3-yn-1-yl)-2-(((2-oxo-2H-chromen-7-yl)oxy)methyl)acrylamide

925047

KB02-COOH

925144

KB05yne, ≥95%

925136

4,6-Dimethyl-2-(methylsulfinyl)-3-nitropyridine

Code de la classe de stockage

10 - Combustible liquids

Classe de danger pour l'eau (WGK)

WGK 3

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Lot/Batch Number

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Vincent M Crowley et al.
ACS central science, 7(4), 613-623 (2021-06-01)
Covalent ligands are a versatile class of chemical probes and drugs that can target noncanonical sites on proteins and display differentiated pharmacodynamic properties. Chemical proteomic methods have been introduced that leverage electrophilic fragments to globally profile the covalent ligandability of
Kristine Senkane et al.
Angewandte Chemie (International ed. in English), 58(33), 11385-11389 (2019-06-22)
Reversible covalency, achieved with, for instance, highly electron-deficient olefins, offers a compelling strategy to design chemical probes and drugs that benefit from the sustained target engagement afforded by irreversible compounds, while avoiding permanent protein modification. Reversible covalency has mainly been
Xiaoyu Zhang et al.
Nature chemical biology, 15(7), 737-746 (2019-06-19)
Ligand-dependent protein degradation has emerged as a compelling strategy to pharmacologically control the protein content of cells. So far, however, only a limited number of E3 ligases have been found to support this process. Here, we use a chemical proteomic

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