SML3179

Homer

≥95% (HPLC)

• Sinónimos: 6-Hydroxy-N-(4’-((5-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-5-oxopentyl)carbamoyl)-4-(4-methylpiperazin-1-yl)-[1,1’-biphenyl]-3-yl)-4-(trifluoromethyl)-nicotinamide, N-(4′-(5-((S)-1-((2S,4R)-4-Hydroxy-2-(4-(4-methylthiazol-5-yl)benzylcarbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-ylamino)-5-oxopentylcarbamoyl)-4-(4-methylpiperazin-1-yl)biphenyl-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide, WD40 repeat domain protein 5 (WDR5) degrader 8g, WDR5 Degrader 8g, WDR5 PROTAC 8g
• Fórmula empírica (notación de Hill): C₅₂H₆₀F₃N₉O₇S
• Número de CAS: 2737222-94-3
• Peso molecular: 1012.15
• Código UNSPSC: 12352107
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: powder
• color: white to beige
• solubilidad: DMSO: 2 mg/mL, clear
• temp. de almacenamiento: 2-8°C
• cadena SMILES: CN1CCN(CC1)C2=C(NC(C3=CNC(C=C3C(F)(F)F)=O)=O)C=C(C4=CC=C(C(NCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C=C6)C7=C(C)N=CS7)=O)=O)=O)=O)C=C4)C=C2

Descripción

Acciones bioquímicas o fisiológicas

Homer (WDR5 Degrader 8g) is a cell-permeable highly efficacious and potent WDR5-selective heterobifunctional degrader composed of WDR5 antagonist OICR-9429 analog plus a butyl chain spacer linked to an E3 ubiquitin ligase von Hippel-Lindau (VHL)-binding ligand that effectively depletes WDR5 in various cancer cell lines (Dmax = 58% and DC50 = 53 nM in MV4-11WDR5-HiBiT cells, 24 h). Homer is shown to dose-dependently induce WDR5 ubiquitylation and proteasomal degradation (Kd = 18 nM; IC50 cellular & lysate = 13.6 & 2.15 μM, respectively, NanoBRET assay).

cell-permeable highly efficacious and potent WDR5-selective heterobifunctional degrader

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable