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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- Formule: C50H52ClN9O7S
- Masse moléculaire:958.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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.
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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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Masse moléculaire 958.52
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YT117R Related Classifications
HY-169148 Related Classifications
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