SML1272

I-BET762

≥98% (HPLC)

• Sinônimo(s): (4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, GSK525762, GSK525762A, I-BET
• Fórmula empírica (Notação de Hill): C₂₂H₂₂ClN₅O₂
• Número CAS: 1260907-17-2
• Peso molecular: 423.90
• Número MDL: MFCD22417091
• Código UNSPSC: 12352200
• ID de substância PubChem: 329825759
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• Formulário: powder
• atividade óptica: [α]/D +80 to +90°, c = 0.3 in methanol
• controle de medicamentos: regulated under CDSA - not available from Sigma-Aldrich Canada
• cor: white to beige
• solubilidade: DMSO: 10 mg/mL, clear
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: CCNC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(OC)=CC=C3N4C1=NN=C4C)=O
• InChI: 1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
• chave InChI: AAAQFGUYHFJNHI-SFHVURJKSA-N
• Informações sobre genes: human ... BRD2(6046) , BRD3(8019) , BRD4(23476) , BRDT(676)

Descrição

Ações bioquímicas/fisiológicas

I-BET762 (GSK525762) is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins BRD2, BRD3 and BRD4 with IC₅₀ values of 32.5–42.5 nM and no interaction with other bromodomain-containing proteins. I-BET mimicks acetylated histone, preventing the protein-protein interaction between acetyl-lysines and the BET reader protein. This was shown to block expression of inflammatory genes in activated macrophages and confer protection against endotoxic shock and bacterial sepsis. I-BET762 also showed potent anti-myeloma activity in vitro and in vivo.

I-BET762 is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins; synthetic histone mimic.

I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression.[1] I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.[2]

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable