BRD4 degrader AT1
CAS No. : 2098836-45-2
| Size | Price | Stock |
|---|---|---|
| 1mg | $161 | In-stock |
| 5mg | $340 | In-stock |
| 10mg | $590 | In-stock |
| 25mg | $1200 | In-stock |
| 50mg | $2100 | In-stock |
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| Cat. No. : | HY-111433 |
| M.Wt: | 972.68 |
| Formula: | C48H58ClN9O5S3 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
BRD4 degrader AT1 is a selective PROTAC BRD4 degrader. BRD4 degrader AT1 induces depletion of Brd4 protein in cells. BRD4 degrader AT1 exhibits highly selective depletion of Brd4 over Brd2 and Brd3 in cells[1].
IC50 & Target:Kd: 44 nM (Brd4BD2, cell assay), 38.8 nM (Brd4BD2 QVK, cell assay), 111 nM (Brd2BD1, cell assay), 94 nM (Brd2BD2, cell assay), 35 nM (Brd3BD1, cell assay), 39 nM (Brd3BD2, cell assay), 75 nM (Brd4BD1, cell assay), 35 nM (Brd2BD1 KEA, cell assay)[1]
In Vitro:BRD4 degrader AT1 drives the formation of a positively cooperative ternary complex with VCB and BET bromodomains, among which the Brd4BD2:AT1:VCB complex exhibits the highest cooperativity and stability[1].
BRD4 degrader AT1 (0.01-3 μM; 24 h) potently and selectively depletes Brd4 protein, with no significant effect on the levels of Brd2 or Brd3[1].
BRD4 degrader AT1 (24 h) selectively depletes Brd4 levels to approximately 40% of the baseline in HeLa cells, with no significant effects on Brd2, Brd3, or the vast majority of other detected cellular proteins[1].
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