2010159-47-2
Chemical Structure
MZP-54
- CAS No.: 2010159-47-2
- Formula:C55H66ClN7O9S
- Molecular Weight:1036.67
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)-15-(tert-butyl)-1,13-dioxo-5,8,11-trioxa-2,14-diazahexadecan-16-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
InChIKey: FYSWLIFIYIVHPI-DDWISSAJSA-N
SMILES: O=C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)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
Biological Activity: MZP-54 is a PROTAC degrader that selectively targets BRD3/BRD4, with a DC50 of < 0.05 μM in AML cells. MZP-54 recruits VHL to form a ternary complex, induces BRD3/BRD4 degradation via the ubiquitin-proteasome pathway, inhibits c-Myc expression, and exerts antiproliferative activity. MZP-54 can be used for the research of acute myeloid leukemia[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MZP-54 | 98.03% | MZP-54 is a PROTAC degrader that selectively targets BRD3/BRD4, with a DC50 of < 0.05 μM in AML cells. MZP-54 recruits VHL to form a ternary complex, induces BRD3/BRD4 degradation via the ubiquitin-proteasome pathway, inhibits c-Myc expression, and exerts antiproliferative activity. MZP-54 can be used for the research of acute myeloid leukemia. | ||||||||||||||||||||
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References
- [1]. Kabir M, et al. Chemically induced degradation of epigenetic targets. Chemical Society reviews. 2023 Jul 03;52(13):4313-4342. [Content Brief]
- [2]. García Jiménez D, et al. Designing Soluble PROTACs: Strategies and Preliminary Guidelines. Journal of medicinal chemistry. 2022 Oct 13;65(19):12639-12649.
- [3]. 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]
