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Merck
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文件

925225

Sigma-Aldrich

KB02yne

同義詞:

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

經驗公式（希爾表示法）:
C17H20ClNO2
CAS號碼:
2376152-06-4
分子量：:
305.80
分類程式碼代碼:
12352101
NACRES:
NA.22

形狀

powder or crystals (or Solid or Liquid)

品質等級

100

反應適用性

reagent type: chemical modification reagent
reaction type: click chemistry

儲存溫度

2-8°C

相關類別

應用

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

其他說明

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

儲存類別代碼

10 - Combustible liquids

水污染物質分類（WGK）

WGK 3

分析證明 (COA)

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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
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
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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