PROTAC TBK1 degrader-2
CAS No. : 2052306-13-3
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| 5mg | $1034 | In-stock |
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| Cat. No. : | HY-112557 |
| M.Wt: | 1093.18 |
| Formula: | C53H74BrN9O9S |
| Purity: | >98 % |
| Solubility: | DMSO : 110 mg/mL (ultrasonic;warming) |
PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM)[1].
IC50 & Target:IC50: 1.3 nM (TBK1), 8.7 nM (IKKε)[1]
In Vitro: PROTAC TBK1 degrader-2 (compound 3i) (100 nM) mediates degradation of TBK1 abrogated by VHL ligand 2 (10 μM) or proteasome inhibitor Carfilzomib (HY-10455) (100 nM)[1].
PROTAC TBK1 degrader-2 (0-3 μM) exhibits poor selectivity for TBK1 over IKKε (IC50 of 1.3 nM vs 8.7 nM), but has no effect on the levels of IKKε, at concentrations of more than 50-fold above its TBK1 DC50[1].
PROTAC TBK1 degrader-2 (100 nM; 300 M; 72 h) is not synthetically lethal in K-Ras mutant versus wild type cells[1].
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