For research use only. Not for therapeutic Use.
Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 , conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (K<sub>d</sub> = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 in cells at 10-100 nM concentrations. DC<sub>50</sub> 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 <em>MYC</em> and upregulation of genes such as <em>P21</em> and <em>AREG</em>. No significant effect on HIF-α stabilization when used at low concentrations (<10 μM).
| Catalog Number | I011385 |
| CAS Number | 1797406-69-9 |
| Synonyms | (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-carboxamid |
| Molecular Formula | C49H60ClN9O8S2 |
| Purity | ≥95% |
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| Storage | Store at -20°C |
