LYN-1604

LYN-1604 is an activator of unc-51-like kinase 1 (ULK1, EC50 = 18.94 nM). It increases Beclin 1, LC3-II, and total LC3 protein levels and reduces levels of p62 in human MDA-MB-231 triple-negative breast cancer (TNBC) cells in a concentration-dependent manner, indicating an increase in autophagy. It also increases the cleavage of the pro-apoptotic protein caspase-3. LYN-1604 decreases the viability of MDA-MB-231 cells in vitro (IC50 = 1.66 µM), an effect that can be reversed by the autophagy inhibitor 3-methyladenine (3-MA, Cay-13242). LYN-1604 (25, 50, and 100 mg/kg) reduces tumor growth in an MDA-MB-231 mouse xenograft model.Formal Name: 2-[bis(2-methylpropyl)amino]-1-[4-[2-(2,4-dichlorophenyl)-2-(2-naphthalenylmethoxy)ethyl]-1-piperazinyl]-ethanone. CAS Number: 2088939-99-3. Molecular Formula: C33H43Cl2N3O2. Formula Weight: 584.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 226 nm. SMILES: O=C(CN(CC(C)C)CC(C)C)N(CC1)CCN1CC(C2=CC=C(Cl)C=C2Cl)OCC3=CC4=CC=CC=C4C=C3. InChi Code: InChI=1S/C33H43Cl2N3O2/c1-24(2)19-37(20-25(3)4)22-33(39)38-15-13-36(14-16-38)21-32(30-12-11-29(34)18-31(30)35)40-23-26-9-10-27-7-5-6-8-28(27)17-26/h5-12,17-18,24-25,32H,13-16,19-23H2,1-4H3. InChi Key: DVNVYWLKGWAELS-UHFFFAOYSA-N.