| Bioactivity | GNE-064 (compound 5) 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[1]. | ||||||||||||
| Target | IC50: 0.035 μM (SMARCA4) | ||||||||||||
| Invitro | GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | GNE-064 (compound 5) (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice [1]. Animal Model: | ||||||||||||
| Name | GNE-064 | ||||||||||||
| CAS | 1997321-20-6 | ||||||||||||
| Formula | C17H21N5O2 | ||||||||||||
| Molar Mass | 327.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Taylor AM, et al. GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. J Med Chem. 2022 Aug 5. |