Home Autophagy ULK agonist - Autophagy agonist LYN-1604 For research use only.

LYN-1604

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). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.

LYN-1604 Chemical Structure

LYN-1604 Chemical Structure

CAS: 2088939-99-3

Selleck's LYN-1604 has been cited by 3 publications

Purity & Quality Control

Batch: S859701 Water] 100 mg/mL] false] Ethanol] 100 mg/mL] false] DMSO] 50 mg/mL] false Purity: 99.36%
99.36

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Biological Activity

Description 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). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Targets
ULK1 [1]
18.94 nM(EC50)
In vitro
In vitro 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[1].
Cell Research Cell lines MDA-MB-231 cells
Concentrations 0.5, 1.0 and 2.0 μM
Incubation Time 24 h
Method

Cells are dispensed in 96-well plates at a density of 5 × 104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of compounds for the indicated time periods. Cell viability is measured by the MTT assay.
In Vivo
In vivo 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 triple negative breast cancer (TNBC) in vitro and in vivo[1].
Animal Research Animal Models MDA-MB-231 xenograft model (BALB/c nude mice)
Dosages 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration intragastric administration

Chemical Information & Solubility

Molecular Weight 657.54 Formula

C33H45Cl4N3O2
CAS No. 2088939-99-3 SDF Download LYN-1604 SDF
Smiles CC(C)CN(CC(C)C)CC(=O)N1CCN(CC1)CC(C2=C(C=C(C=C2)Cl)Cl)OCC3=CC4=CC=CC=C4C=C3
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL

Ethanol : 100 mg/mL

DMSO : 50 mg/mL ( (76.04 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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