Chemical Structure : GNE-049
CAS No.: 1936421-41-8
货号: 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.
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5 mg | ¥3280 | In stock | |
10 mg | ¥5280 | In stock | |
25 mg | ¥8580 | 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.
分子量 | 510.59 | |
分子式 | C27H32F2N6O2 | |
外观性状 | Solid | |
储存条件 |
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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 |
1. Jin L, et al. Cancer Res. 2017 Aug 17. pii: canres.0314.2017.
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