[CAS NO. 2088939-99-3] LYN-1604
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PRODUCTS SPECIFICATIONS [2088939-99-3]
Catalog
SLK-S8597
Brand
Selleck
CAS
2088939-99-3
DESCRIPTION [2088939-99-3]
Overview
| MDL | MFCD31619235 |
|---|---|
| Molecular Weight | 657.54 |
| Molecular Formula | C33H45Cl4N3O2 |
| SMILES | ClC1=CC=C(C(OCC2=CC=C3C=CC=CC3=C2)CN4CCN(C(CN(CC(C)C)CC(C)C)=O)CC4)C(Cl)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
LYN-1604 is a potential agonist with of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (=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
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.
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.
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