autophagic

Clarithromycin (A-56268) is a Macrolide Antimicrobial. The mechanism of action of clarithromycin is as a Cytochrome P450 3A4 Inhibitor, and Cytochrome P450 3A Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of clarithromycin is Macrolides.

1. Liensinine, a kind of isoquinoline alkaloid, can antagonize the ventricular arrhythmias.

Indomethacin farnesil (Infree) is a prodrug of indomethacin. It acts as a nonsteroidal anti-inflammatory drug (NSAID) and disease-modifying anti-rheumatic drug (DMARD).

BL-918 is a potent activator of UNC-51-like kinase 1 (ULK1) with an EC50 of 24.14 nM.

GW406108X (GW108X) is a Kif15 inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X is also an ULK1 kinase inhibitor with pIC50 values of 6.37 (427 nM) and block autophagic flux.

CDK9 autophagic degrader 1 (Compound 28) is an ATTEC degrader used to target and degrade CDK9, also impacting the levels of its associated Cyclin T1. At a concentration of 100 nM, it exhibits over 80% inhibition of CDK9.

PCSK9 autophagic degrader 2 (W6) is an autophagosome-targeting agent for PCSK9, with a DC50 value of 20.6 nM. It exhibits effects comparable to anti-atherosclerotic treatments and has a binding constant (KD) with LC3B of 2.5 μM.

PDEδ autophagic degrader 1 (compound 12c) is an autophagosome-tethering compound (ATTEC) and a potent autophagic degrader of PDEδ. This compound effectively reduces PDEδ protein levels through lysosome-mediated autophagy without affecting PDEδ mRNA expression. Additionally, PDEδ autophagic degrader 1 inhibits the growth of KRAS mutant pancreatic cancer cells.

EACC, a reversible autophagy inhibitor, selectively impedes Stx17, an autophagosome-specific SNARE, from translocating, hence obstructing the fusion between autophagosomes and lysosomes. This compound effectively halts autophagic flux.

HJ-PI01 (HJ-PI01) is a Pim-2 inhibitor. HJ-PI01 (HJ-PI01) induces apoptosis and autophagic cell death in triple-negative human breast cancer.

N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with anti-melanoma activity. N6-Isopentenyladenosine, an RNA modification found in cytokinins, regulates plant growth/differentiation and improves the efficiency

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons. MPP+ induces autophagic cell death in SH-SY5Y cells.

LV-320 is a potent, uncompetitive ATG4B inhibitor with an IC50 of 24.5 μM and a Kd of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic, and active in vivo. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1].

SW063058 is an autophagy inducer that specifically disrupts the interaction between Beclin 1 and Bcl-2 without affecting the interactions of Bcl-2 with pro-apoptotic members (such as Bax and BIM). By inhibiting the negative regulation of Beclin 1 (key to autophagy initiation) by Bcl-2, SW063058 enhances autophagic activity without inducing cytotoxicity, apoptosis, or other forms of cell death in vitro.

YT 6-2 is an autophagy-targeting ligand (ATL) aimed at p62/SQSTM1, used in the synthesis of AUTOTAC degrader ATC-324. ATC-324 induces the formation of AR/p62 complexes, leading to the autophagic-lysosomal degradation of AR. It reduces nuclear AR levels, downregulates the expression of AR and AR-v7 target genes, and also degrades common AR mutants in PCa.

YT 6-2 analog-1 (compound 2-3) serves as an autophagy-targeting ligand (ATL) aimed at p62/SQSTM1, useful in synthesizing the AUTOTAC degrader ATC-324 for the Androgen Receptor (AR). ATC-324 promotes the formation of AR/p62 complexes, leading to the autophagic-lysosomal degradation of AR. It effectively reduces nuclear AR levels, downregulates the expression of AR and AR-v7 target genes, and can degrade common AR mutants found in prostate cancer (PCa).

PBA-1105 TFA is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. This compound selectively binds to the exposed hydrophobic regions of misfolded proteins, promoting their degradation through the autophagy (autophagy) pathway. Additionally, PBA-1105 TFA enhances the autophagic flux of Ub-bound aggregates.

1,3-Propanediol-SNS-032 is a conjugate of a target protein ligand and linker, utilized in the synthesis of PROTACCDK9 autophagic degrader 1.

LC3B ligand 1 is the target protein ligand for PROTAC, and it can be utilized in the synthesis of PROTACCDK9 autophagic degrader 1.

PCSK9ligand 2 is the target protein ligand of PROTACPCSK9 autophagic degrader 2, and it is applicable for research related to anti-atherosclerosis.

LC3B ligand 2 is a ligand for E3 ubiquitin ligase. It can be connected to a target protein ligand through a linker, forming PROTACPCSK9 autophagic degrader 2. PROTACs are capable of inducing the ubiquitination and degradation of oncogenic proteins.

ATC-324 is a potent autophagy-targeting chimera (AUTOTAC) degrader of the androgen receptor (AR) with a DC50 of 2.05 µM. It induces autophagic-lysosomal degradation of AR, decreases nuclear AR and AR-V7 activity, and exhibits cytotoxic effects on AR-positive prostate cancer cells, making it useful for prostate cancer research.

MC2646 is an effective antiparasitic agent that induces autophagy (autophagic) and activates the AMPK/TFEB pathway.

STL001 is a potent and selective inhibitor of FOXM1. It triggers the translocation of nuclear FOXM1 to the cytoplasm, promoting autophagic degradation. STL001 enhances the sensitivity of human cancers to broad-spectrum cancer therapies.