2018年5月17日星期四

LYN-1604||LYN1604|CAS: 2088939-99-3

LYN-1604||LYN1604|CAS: 2088939-99-3

DC Chemicals, Website:www.dcchemicals.com

Product Name: LYN-1604|CAS: 2088939-99-3|Cat No: DC10715|Other Names: LYN-1604,LYN 1604,LYN1604

LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM).

LYN-1604 is a ULK1 agonist. Three amino acid residues (LYS50, LEU53, and TYR89) are key to the activation site of LYN-1604 and ULK1 by site-directed mutagenesis and biochemical assays. LYN-1604 induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 is bound to wild-type ULK1 with a binding affinity in the nanomole range (KD = 291.4 nM), but the ULK1Y89A mutant protein causes a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1K50A and ULK1L53A mutants.LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. LYN-1604 can directly activate ULK1, the initiator of autophagy, thereby inducing cell death to inhibit the growth of TNBC in vitro and in vivo.


没有评论:

发表评论