| Name | MZ 1 |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 0567 |
| Cas Number | 1797406-69-9 |
| Chemical Name | (2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Formula | C49H60ClN9O8S2 |
| Molecular Weight | 1002.64 |
| Purity | >98 % |
| Description | Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 (Cat.No. 4499), conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (K d = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 in cells at 10-100 nM concentrations. DC 50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively. Replicates the effects of BRD4 protein removal by siRNA altering downstream gene expression patterns: downregulation of MYC and upregulation of genes such as P21 and AREG . No significant effect on HIF-α stabilization when used at low concentrations (<10 μM). Exhibits potent cytotoxicity and profound antiproliferative effects in AML cell lines such as Mv4;11 (pEC50 = 7.6), more potent and more effective than (+)-JQ1 (pEC50 = 6.5). Negative control cis MZ 1 also available. PROTACs are bi-functional small molecules that harness the ubiquitin/proteasome system (UPS) to selectively and catalytically remove target proteins from cells. |
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