WDR5-IN-6 is a WDR5 inhibitor, targeting to WBM site. WDR5-IN-6 inhibits cell proliferation of neuroblastoma cell lines with potent anti-tumor activity. WDR5-IN-6 shows high synergy with OICR-9429 , a WDR5 inhibitor targeting to WIN site. WDR5-IN-6 can be used for reasearch in neuroblastoma.
WDR5-IN-6 (compound 19) inhibits the proliferation of IMR32 and LAN5 cells with EC50 values of 12.34 and 14.89 μM, respectively. WDR5-IN-6 shows moderate inhibitory effect on SK-N-AS cells, without effect on HEK293T cells at 20 μM[1].
References:
[1]. Han QL, et al. Discovery, evaluation and mechanism study of WDR5-targeted small molecular inhibitors for neuroblastoma. Acta Pharmacol Sin. 2023 Apr;44(4):877-887.