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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- 分子式: C50H52ClN9O7S
- 分子量:958.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
BRD4 |
体外実験
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.
化学情報
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分子量 958.52
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
YT117R 関連分類
HY-169148 関連分類
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