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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-WDR5 oligomerization inducer WZ-1
WDR5 oligomerization inducer WZ-1

Chemical Structure : WDR5 oligomerization inducer WZ-1

CAS No.: 681855-03-8

WDR5 oligomerization inducer WZ-1

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 483.46
分子式 C18H12Cl2N4S4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5,5'-disulfanediylbis(4-(4-chlorophenyl)thiazol-2-amine)

参考文献

1. Fang Y, et al. Nat Commun. 2026 Mar 13. doi: 10.1038/s41467-026-70409-z.

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