2088939-99-3

Basic information

• Product Name: LYN-1604
• Synonyms: LYN-1604;LYN-1604 Hcl
• CAS NO: 2088939-99-3
• Molecular Formula: C33H45Cl4N3O2
• Molecular Weight: 657.5413
• EINECS: -0
• Mol File: 2088939-99-3.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: LYN-1604(CAS DataBase Reference)
• NIST Chemistry Reference: LYN-1604(2088939-99-3)
• EPA Substance Registry System: LYN-1604(2088939-99-3)

Safety Data

• Hazardous Substances Data: 2088939-99-3(Hazardous Substances Data)

Usage

Uses

Used in Anticancer Applications:
LYN-1604 is used as an anticancer agent for its ability to increase autophagy and induce apoptosis in human MDA-MB-231 triple-negative breast cancer cells. It reduces tumor growth in an MDA-MB-231 mouse xenograft model, making it a promising candidate for cancer treatment.
Used in Pharmaceutical Research:
LYN-1604 is used as a research tool for studying the role of autophagy and apoptosis in cancer cell death. Its ability to modulate these processes can provide valuable insights into the development of novel cancer therapies.
Used in Drug Development:
LYN-1604 is used as a potential drug candidate for the development of new cancer treatments, particularly for triple-negative breast cancer, due to its demonstrated efficacy in reducing tumor growth and inducing cell death.

Upstream product

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Relevant articles and documents

ULK1 micromolecule stimulant and application of stimulant in antitumor drug

The invention relates to an ULK1 micromolecule stimulant and an application of the stimulant in an antitumor drug, which belong to the technical field of antitumor pharmacy. The invention provides a compound taken as the ULK1 micromolecule stimulant. The compound comprises the compound shown in a specification or its pharmaceutically acceptable salt. The compound or its pharmaceutically acceptable salt can be taken as the ULK1 stimulant, has certain antineoplastic activity, and effectively inhibits the growth of the cancer cells. The compound has obvious inhibition effect for a plurality of tumor cells, especially breast cancer cells.

Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo

UNC-51-like kinase 1 (ULK1) is well-known to initiate autophagy, and the downregulation of ULK1 has been found in most breast cancer tissues. Thus, the activation of ULK1-modulated autophagy could be a promising strategy for breast cancer therapy. In this study, we found that ULK1 was remarkably downregulated in breast cancer tissue samples by The Cancer Genome Atlas (TCGA) analysis and tissue microarray (TMA) analysis, especially in triple negative breast cancer (TNBC). To design a ULK1 agonist, we integrated in silico screening and chemical synthesis to acquire a series of small molecule candidates. After rounds of kinase and anti-proliferative activity screening, we discovered the small molecule, LYN-1604, to be the best candidate for a ULK1 agonist. Additionally, we identified that three amino acid residues (LYS50, LEU53, and TYR89) were key to the activation site of LYN-1604 and ULK1 by site-directed mutagenesis and biochemical assays. Subsequently, we demonstrated that LYN-1604 could induce cell death, associated with autophagy by the ULK complex (ULK1-mATG13-FIP200-ATG101) in MDA-MB-231 cells. To further explore LYN-1604-induced autophagic mechanisms, we found some potential ULK1 interactors, such as ATF3, RAD21, and caspase3, by performing comparative microarray analysis. Intriguingly, we found that LYN-1604 induced cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. Moreover, we demonstrated that LYN-1604 has potential for good therapeutic effects on TNBC by targeting ULK1-modulated cell death in vivo; thus making this ULK1 agonist a novel potential small-molecule drug candidate for future TNBC therapy.