Chemical Structure : WDR5 oligomerization inducer WZ-1
CAS No.:
681855-03-8
WDR5 oligomerization inducer WZ-1
Catalog No.: PC-26366Not For Human Use, Lab Use Only.
WZ-1 is a selective WDR5 oligomerization inducer, binds the WBM site of WDR5 and reacts with Cys248 to form an intramolecular disulfide, triggers oligomerization via thio-disulfide exchange, disrupting WDR5 interactions at both WIN and WBM sites.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
WZ-1 is a selective WDR5 oligomerization inducer, binds the WBM site of WDR5 and reacts with Cys248 to form an intramolecular disulfide, triggers oligomerization via thio-disulfide exchange, disrupting WDR5 interactions at both WIN and WBM sites.
WZ-1 inhibits cancer cell proliferation of colon cancer cell lines: CT26, RKO, DLD1, and SW620, with IC50 of 1.1-6.2 uM, by disrupting the interaction between WDR5 and its partner proteins.
WZ-1 does not substantially inhibit proliferation in normal colon cell lines NCM460 and immortalized human colon fibroblasts.
WZ-1 caused G0/G1 phase cell cycle arrest, induces significant negative enrichment of E2F and G2M checkpoint signaling pathways on CT26 cells.
WZ-1 also inhibits the expression of Myc target genes, markedly disrupts WDR5 binding to both MLL1 and c-Myc.
Physicochemical Properties
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M.Wt
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483.46
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Formula
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C18H12Cl2N4S4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5,5'-disulfanediylbis(4-(4-chlorophenyl)thiazol-2-amine)
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References
1. Fang Y, et al. Nat Commun. 2026 Mar 13. doi: 10.1038/s41467-026-70409-z.
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