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GNE-064
CAS No. 1997321-20-6
GNE-064( —— )
Catalog No. M35320 CAS No. 1997321-20-6
GNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 88 | In Stock |
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| 5MG | 85 | In Stock |
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| 10MG | 136 | In Stock |
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| 25MG | 226 | In Stock |
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| 50MG | 316 | In Stock |
|
| 100MG | 429 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGNE-064
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NoteResearch use only, not for human use.
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Brief DescriptionGNE-064 is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5.
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DescriptionGNE-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.
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In VitroGNE-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.
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In VivoGNE-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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Synonyms——
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PathwayChromatin/Epigenetic
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TargetEpigenetic Reader Domain
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RecptorEpigenetic Reader Domain
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Research Area——
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Indication——
Chemical Information
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CAS Number1997321-20-6
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Formula Weight327.38
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Molecular FormulaC17H21N5O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 125 mg/mL (381.82 mM)
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SMILESC[C@@H]1CN(CCN1C(C)=O)c1cc(nnc1N)-c1ccccc1O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
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.?
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