LYN-1604 hydrochloride

LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).

Product information

CAS Number: 2216753-86-3

Molecular Weight: 621.08

Formula: C33H44Cl3N3O2

Chemical Name: 2-[bis(2-methylpropyl)amino]-1-{4-[2-(2,4-dichlorophenyl)-2-[(naphthalen-2-yl)methoxy]ethyl]piperazin-1-yl}ethan-1-one hydrochloride

Smiles: Cl.CC(C)CN(CC(=O)N1CCN(CC(OCC2C=C3C=CC=CC3=CC=2)C2=CC=C(Cl)C=C2Cl)CC1)CC(C)C

InChiKey: KWFDUNOLEJSFBQ-UHFFFAOYSA-N

InChi: InChI=1S/C33H43Cl2N3O2.ClH/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;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (161.01 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) . LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) . LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells. LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells. LYN-1604 induces ATG5-dependent autophagy via the ULK complex. LYN-1604 can also increase cleavage of caspase3 and induce apoptosis.

In Vivo:

LYN-1604 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg; intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death.

Products are for research use only. Not for human use.