2010159-48-3
Chemical Structure
MZP-55
- CAS No.: 2010159-48-3
- Formula:C57H70ClN7O10S
- Molecular Weight:1080.72
IUPAC Name: (2S,4R)-1-((S)-1-(4-((2S,4R)-1-acetyl-4-((4-chlorophenyl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)phenyl)-18-(tert-butyl)-1,16-dioxo-5,8,11,14-tetraoxa-2,17-diazanonadecan-19-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
InChIKey: UHWNJFZTYJNBAN-HYXXSBGTSA-N
SMILES: CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCNC(C(C=C4)=CC=C4C5=CC6=C(C=C5)N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7)=O)=O)=O)=O)C=C2
Biological Activity: MZP-55 is a BRD4 BD2 PROTAC degrader with a Kd value of 8 nM; its pDC50 values are 8.1 (short isoform) and 7.5 (long isoform), respectively. MZP-55 mediates the negatively cooperative formation of the Brd4BD2-VCB ternary complex, with Kd values of 109 nM and 183 nM for the VCB protein complex and the ternary complex, respectively. MZP-55 drives cMyc depletion and induces antiproliferative activity. MZP-55 can be used in the research of acute myeloid leukemia[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MZP-55 | 99.94% | MZP-55 is a BRD4 BD2 PROTAC degrader with a Kd value of 8 nM; its pDC50 values are 8.1 (short isoform) and 7.5 (long isoform), respectively. MZP-55 mediates the negatively cooperative formation of the Brd4BD2-VCB ternary complex, with Kd values of 109 nM and 183 nM for the VCB protein complex and the ternary complex, respectively. MZP-55 drives cMyc depletion and induces antiproliferative activity. MZP-55 can be used in the research of acute myeloid leukemia. | ||||||||||||||||||||
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References
- [1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. Journal of medicinal chemistry. 2018 Jan 25;61(2):504-513. [Content Brief]
