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Merck

914738

KB02-SLF

≥95%

Synonyme(s) :

(R)-1-(3-(3-(2-(2-(2-((1-(2-Chloroacetyl)-1,2,3,4-tetrahydroquinolin-6-yl)oxy)acetamido)ethoxy)ethoxy)propanamido)phenyl)-3-(3,4-dimethoxyphenyl)propyl (S)-1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate, Electrophilic PROTAC®, Heterobifunctional conjugate for E3 ubiquitin ligase discovery

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A propos de cet article

Formule empirique (notation de Hill) :
C50H65ClN4O12
Numéro CAS:
2384184-40-9
Poids moléculaire :
949.52
MDL number:
MFCD32263417
UNSPSC Code:
12352200
NACRES:
NA.22
Assay:
≥95%
Form:
powder

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ligand

electrophilic fragment

Quality Level

100

assay

≥95%

form

powder

storage temp.

−20°C

SMILES string

O=C(CCl)N1CCCC2=CC(OCC(NCCOCCOCCC(NC3=CC=CC([C@H](OC([C@@H]4CCCCN4C(C(C(C)(C)CC)=O)=O)=O)CCC5=CC(OC)=C(OC)C=C5)=C3)=O)=O)=CC=C21

InChI

1S/C50H65ClN4O12/c1-6-50(2,3)47(59)48(60)55-23-8-7-14-40(55)49(61)67-41(19-15-34-16-20-42(62-4)43(29-34)63-5)36-11-9-13-37(30-36)53-44(56)21-25-64-27-28-65-26-22-52-45(57)33-66-38-17-18-39-35(31-38)12-10-24-54(39)46(58)32-51/h9,11,13,16-18,20,29-31,40-41H

InChI key

OKJBKEQXKMMRPL-WVILEFPPSA-N

Catégories apparentées

Application

KB02-SLF is an electrophilic PROTAC developed in the Cravatt lab and is useful for the discovery of ligandable E3 ligases, an area of interest for the targeted protein degradation (TPD) field seeking to map out and utilize a larger repertoire of the available human E3 ligases. This bifunctional tool compound comprises a synthetic ligand for FKBP12 (SLF) on one end and scout fragment 912131 on the other end. Scout fragments are electrophiles that covalently modify targetable cysteine residues on proteins, an approach that has been scaled to globally quantitate Cys reactivity across human proteomes and cells. When SLF and the electrophilic fragment are fused together, monitoring the levels of FKBP12 in cells may indicate scout-mediated FKBP12 degradation, for which follow-up studies would validate the mechanism of FKPB12 depletion and any targets to which the scout fragment is covalently bound. Scout-bound proteins leading to FKBP12 (or other targets) depletion discovered by this strategy will further expand the communal TPD toolbox. Due to the reactive nature of the scout fragment, other proteins will also be modified, so careful controls and validation should be considered.

This proteomic approach to E3 discovery was demonstrated by Zhang et al in the discovery that DCAF16 mediated nuclear FKBP12 degradation via KB02-SLF.

Additional electrophilic PROTACs were developed incorporating scout fragments with broad cysteine reactivity:
  • KB03-SLF (914975) containing chloroacetamide scout fragment 912654
  • KB05-SLF (913715) containing acrylamide scout fragment 911798


Related tools:
  • Additional bifunctional tools for FKPB12 variants: dTAG-13 (SML2601 for FKBP12F36V) and Biotin-SLF (914223 for FKBP12)
  • Inhibitors useful in validation of proteasomal-mediated degradation: MG123 (SML1135) and MLN4924 (5.05477for Cullin-RING ubiquitin ligases that regulate neddylation of Cullin proteins)
  • Cereblon (CRBN) affinity probe: Biotin-Thalidomide (913979)

Other Notes

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

Technology Spotlight: Proteomic Ligandability Assessment

Technology Spotlight: Building PROTAC® Degraders for Targeted Protein Degradation

Legal Information

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

related product

Réf. du produit
Description
Tarif

SML2601

dTAG-13, ≥98% (HPLC)

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

914223

Biotin-SLF

913979

Biotin-Thalidomide, ≥95%

925047

KB02-COOH

925225

KB02yne

925136

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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

Numéro d'article de commerce international

RéférenceGTIN
914738-5MG04061842093700

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