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Chemical Structure : GNE-781
CAS No.: 1936422-33-1
Catalog No.: PC-60306Not For Human Use, Lab Use Only.
GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $288 | In stock | |
| 10 mg | $458 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.
GNE-781 exhibits high selectivity over BRD4 (1) (>5 uM) and other BRDs.
GNE-781 suppresses Myc transcript levels in cellular assays with EC50 of 6.6 nM.
GNE-781 displays antitumor activity in an AML tumor model and decreases Foxp3 transcript levels in a dose dependent manner.
| M.Wt | 525.605 | |
| Formula | C27H33F2N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-[7-(Difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-N-methyl-1-tetrahydropyran-4-yl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carboxamide |
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1. Romero FA, et al. J Med Chem. 2017 Nov 22;60(22):9162-9183.
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