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GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $35 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $143 | In Stock | |
25 mg | $238 | In Stock | |
50 mg | $340 | In Stock | |
100 mg | $461 | In Stock | |
1 mL x 10 mM (in DMSO) | $93 | In Stock |
Description | GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis. |
In vitro | GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells[1]. |
In vivo | GNE-064 (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice [1]. |
Alias | GNE064 |
Molecular Weight | 327.38 |
Formula | C17H21N5O2 |
Cas No. | 1997321-20-6 |
Smiles | C[C@@H]1CN(CCN1C(C)=O)c1cc(nnc1N)-c1ccccc1O |
Relative Density. | 1.276 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (343.6 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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