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Chemical Structure : GNE-049
CAS No.: 1936421-41-8
Catalog No.: PC-61641Not For Human Use, Lab Use Only.
GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $328 | In stock | |
| 10 mg | $528 | In stock | |
| 25 mg | $858 | In stock | |
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| 100 mg | Get quote |
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GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
GNE-049 displays 3,850-fold selectivity over BRD4.
GNE-049 shows excellent potency (12 nM) in a BRET cellular assay and inhibits the expression of MYC with EC50 of 14 nM in MV-4-11 cells.
GNE-049 demonstrates significant dose-dependent inhibition of AR signaling and PC proliferation in vitro and in vivo.
| M.Wt | 510.59 | |
| Formula | C27H32F2N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one |
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1. Jin L, et al. Cancer Res. 2017 Aug 17. pii: canres.0314.2017.
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