| Chemical Properties | Back Directory | [Boiling point ]
1179.9±65.0 °C(Predicted) | [density ]
1.322±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
8.63±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A)[1]. | [Biological Activity]
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 th at effectively depletes WDR5 in various cancer cell lines (Dmax = 58% and DC50 = 53 nM in MV4-11WDR5-HiBiT cells24 h). Homer is shown to dose-dependently induce WDR5 ubiquitylation and proteasomal degradation (Kd = 18 nM; IC50 cellular & lysate = 13.6 & 2.15 μMrespectivelyNanoBRET assay). | [References]
[1] D?lle A, et al. Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders. J Med Chem. 2021 Aug 12;64(15):10682-10710. DOI:10.1021/acs.jmedchem.1c00146 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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