WDR5-IN-1 - 10mM in DMSO, high purity , CAS No.2408842-51-1(DMSO)

Item Number

W655312

• Specifications & Purity: 10mM in DMSO
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a K d of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC 50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.

In Vitro

WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells. WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels.\nWDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell Line: MV4:11 cells Concentration: 1 µM Incubation Time: 48 hours Result: Showed an approximate 4 fold increased SubG1 cells. Western Blot AnalysisCell Line: MV4:11 cells Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 µM Incubation Time: 24, 48 hours Result: p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h.