产品介绍
Product Description
Biochem/physiol Actions
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
技术参数
Specifications
| Quality Level | 100 |
| assay | ≥95% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | 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 |
