YT117R
YT117R is a PROTAC degrader targeting BRD4. YT117R binds stereoselectively and site-specifically to the cysteine residue C1113 of DCAF1 to form a covalent interaction. YT117R promotes BRD4 degradation via a DCAF1-dependent, proteasome- and cullin-RING E3 ligase-mediated process. YT117R exhibits stereoselective activity dependent on wild-type DCAF1, which is blocked by the DCAF1C1113A mutation.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF1 ligand (HY-158301); Black: linker (HY-42776)).
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- 화학식: C50H52ClN9O7S
- 분자량:958.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
BRD4 |
In Vitro
YT117R stereoselectively engages C1113 of recombinant DCAF1, as shown by concentration-dependent blockade of MY-11B probe labeling in gel-ABPP assays[1].
YT117R (0.05-1 μM; 12 h) induces concentration-dependent, stereoselective, and DCAF1C1113-dependent degradation of BRD4 in DCAF1-WT-expressing HEK293T cells, with an activity dependent on the proteasome and cullin-RING E3 ligase pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:DCAF1-WT-expressing HEK293T cells
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Concentration:0.05 μM; 0.1 μM; 0.2 μM; 0.5 μM; 1 μM
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Incubation Time:12 h
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Result:Promoted concentration-dependent degradation of BRD4 in DCAF1-WT-expressing cells.
Induced submaximal degradation compared to positive control dBET6.
Showed stereoselective activity (not induced by YT117S).
Exhibited absent degradation in DCAF1-C1113A-expressing cells.
Had induced BRD4 degradation blocked by pre-treatment with MLN4924 and MG132.
Chemical Information
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분자량 958.52
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화학식 C50H52ClN9O7S
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SMILES
C=CC(N1C[C@@H]([C@@H]1C(NC2=CC=CC3=C2N=CC=C3)=O)C4=CC=C(C=C4)C(NCCOCCOCCOCCNC(C[C@@H]5N=C(C6=C(N7C(C)=NN=C57)SC(C)=C6C)C8=CC=C(C=C8)Cl)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YT117R Related Classifications
HY-169148 Related Classifications
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