GNE-064

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 IC 50 of 0.035 μM and inhibits SMARCA2 with an EC 50 of 0.10 μM. GNE-064 possess K d s 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 agent synthesis In Vitro GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: ZsGreen-SMARCA2 BD-expressing U2OS cells Concentration: 0-0.5 μM Incubation Time: 1 hour Result: Inhibited SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells with an EC 50 of 0.1 μM. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice Dosage: 0.5 mg/kg (i.v.) and 1.0 mg/kg (p.o.) Administration: Intravenous injection and oral gavage; 0.5 mg/kg and 1.0 mg/kg once Result: Showed a low unbound plasma clearance with 16 mL/min/kg, a reasonable half-life of 1.1 h and good oral bioavailability of 59%. Form:Solid IC50& Target:IC50: 0.035 μM (SMARCA4)

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