MS479
MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells.
(Pink: BRD4 ligand (HY-78695); Blue: SPOP ligand (HY-176036); Black: linker (HY-176037)).
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- Fòrmula: C59H82ClN11O5S
- Peso molecular:1092.87
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
MS479 (Compound 9) (0.5-5 μM, 24 h) shows the best degradation of BRD4 (S) (>50% degradation at 5 μM) in HT29 cell line[1].
MS479 (0.156-10 μM, 24 h) shows relatively weak effect on the BRD4 (L) protein level (DC50 = 13.2 μM), with approximately 50% degradation at 10 μM in HT29 cell line[1].
MS479 (1-10 μM, 24 h) regulates the BRD4 protein level through a post-translational mechanism in HT29 cell line[1].
MS479 (5 μM, 24 h) suggests the degradation of BRD4 (S) is dependent on BRD4, GLP, SPOP, and UPS engagement in HT29 cell line[1].
MS479 (0.021-10 μM, 72 h) displays a significant antiproliferative effect (GI50 = 4.5 μM) in a concentration-dependent manner in HT29 cells but not cytotoxic to normal cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29
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Concentration:1-10 μM
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Incubation Time:2-72 h
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Result:Observed degradation of BRD4 (S) at 16 h and persisted up to 72 h.
Required longer time (48 h or longer) to degrade BRD4 (L), BRD3, and BRD2 effectively.
Reduced c-Myc protein level sharply after 2 h and completely abolished at 16 h.
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Cell Line:Biotin-MS479 (20 or 100 μM), parent BRD4 ligand (JQ1 (HY-13030), 1 μM), parent GLP ligand (MS1262, 1 μM) or a neddylation inhibitor (MLN4924 (HY-70062), 1 μM) pre-treated HT29 cell lines
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Concentration:5 μM
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Incubation Time:24 h
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Result:Rescued BRD4 (S) degradation by pretreatment of HT29 cells.
Induced BRD4 degradation in HT29 cells, but the negative controls (MS479N1 and MS479N2) did not.
Showed BRD4 (S), BRD4 (L), and GLP all coeluted with SPOP in the presence of Biotin MS479, suggesting MS479 indeed induces the interaction between BRD4 and the GLP-SPOP complex.
Chemical Information
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Peso molecular 1092.87
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Fòrmula C59H82ClN11O5S
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SMILES
CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCCCCCCCCCNC(CCCN5CCC(NC6=C7C=C(OC)C(OCCCN8CCCC8)=CC7=NC(N9CCOCC9)=C6)CC5)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS479 Related Classifications
HY-176035 Related Classifications
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