GNE-064

Research use only, not for human use.

GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5.

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 agent synthesis.

GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells.Cell Viability Assay Cell 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 EC50 of 0.1 μM.

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 .Animal Model:Female CD-1 miceDosage: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%.

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Chromatin/Epigenetic

Epigenetic Reader Domain

Epigenetic Reader Domain

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1997321-20-6

327.38

C17H21N5O2

>98% (HPLC)

In Vitro:?DMSO : ≥ 125 mg/mL (381.82 mM)

C[C@@H]1CN(CCN1C(C)=O)c1cc(nnc1N)-c1ccccc1O

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(-20℃)

With Ice Pack

≥ 2 years