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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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M651024-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $850.90 | |
M651024-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,600.90 | |
M651024-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $550.90 |
Synonyms | MZP-54 | 2010159-47-2 | CHEMBL4229193 | (2S,4R)-1-[(2S)-2-[[2-[2-[2-[2-[[4-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoyl]amino]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5 |
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Specifications & Purity | ≥98% |
Biochemical and Physiological Mechanisms | MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4 , with a K d of 4 nM for Brd4 BD2 . |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4 , with a K d of 4 nM for Brd4 BD2 . In Vitro MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a K d of 4 nM for Brd4 BD2 . MZP-54 binds to VHL-EloC-EloB protein (VCB) with a K d of 105 ± 24 nM. MZP-54 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC 50 s of 7.08 ± 0.05 and 6.37 ± 0.03, respectively. MZP-54 also exhibits high depletion of cMyc levels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:VHL BRD4 BD2 4 nM (Kd) |
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IUPAC Name | (2S,4R)-1-[(2S)-2-[[2-[2-[2-[2-[[4-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoyl]amino]ethoxy]ethoxy]ethoxy]acetyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide |
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INCHI | InChI=1S/C55H66ClN7O9S/c1-34-27-46(60-43-18-16-42(56)17-19-43)45-28-41(15-20-47(45)63(34)36(3)64)38-11-13-40(14-12-38)52(67)57-21-22-70-23-24-71-25-26-72-32-49(66)61-51(55(4,5)6)54(69)62-31-44(65)29-48(62)53(68)58-30-37-7-9-39(10-8-37)50-35(2)59-33-73-50/h7-20,28,33-34,44,46,48,51,60,65H,21-27,29-32H2,1-6H3,(H,57,67)(H,58,68)(H,61,66)/t34-,44+,46+,48-,51+/m0/s1 |
InChi Key | FYSWLIFIYIVHPI-DDWISSAJSA-N |
Canonical SMILES | CC1CC(C2=C(N1C(=O)C)C=CC(=C2)C3=CC=C(C=C3)C(=O)NCCOCCOCCOCC(=O)NC(C(=O)N4CC(CC4C(=O)NCC5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)NC7=CC=C(C=C7)Cl |
Isomeric SMILES | C[C@H]1C[C@H](C2=C(N1C(=O)C)C=CC(=C2)C3=CC=C(C=C3)C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N4C[C@@H](C[C@H]4C(=O)NCC5=CC=C(C=C5)C6=C(N=CS6)C)O)C(C)(C)C)NC7=CC=C(C=C7)Cl |
Alternate CAS | 2010159-47-2 |
PubChem CID | 122551841 |
Molecular Weight | 1036.67 |
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Solubility | Ethanol : 50 mg/mL (48.23 mM; Need ultrasonic) |
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