WDR5-IN-1 |
| Catalog No.GC62558 |
WDR5-IN-1 es un inhibidor potente y selectivo del dominio 5 de repeticiÓn de WD (WDR5), con una Kd de <0,02 nM. WDR5-IN-1 inhibe la actividad de la histona metiltransferasa (HMT) de MLL1 con una IC50 de 2,2 nM. WDR5-IN-1 disminuye el reclutamiento de MYC en los genes desplazados por WDR5 y muestra potentes efectos antiproliferativos en las lÍneas CHP-134 (neuroblastoma) y Ramos (linfoma de Burkitt).
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Cas No.: 2408842-51-1
Sample solution is provided at 25 µL, 10mM.
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WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 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[1].
WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1].WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1].WDR5-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[1].
[1]. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675.
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