质量水平
方案
≥95% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
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
生化/生理作用
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
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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