autophagic

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

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.

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.

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. Oleandrin (Folinerin), the principal cardiac glycoside component of PBI-524, can quantitatively account for regulation of BDNF at both the protein and transcriptional levels. 2. Oleandrin are known to inhibit the Na, K-ATPase pump, resulting in a consequent increase in calcium influx in heart muscle. 3. Oleandrin has stronger anti-proliferative activity in undifferentiated CaCO-2 cells (IC50, 8.25 nM) , causes an autophagic cell death and altered ERK phosphorylation in undifferentiated.

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.

CAA0225 is a selective inhibitor of cathepsin L. CAA0225 is a probe for autophagic proteolysis.

DHA-37 is an inducer of autophagic cell death through upregulation of HMGB1 in A549 cells.

OAB-14 is a Bexarotene derivative that improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal(EAL) pathway in APP/PS1 transgenic mice [1] [2].

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0/G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells.

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

Alisol A (Alisol-A) may be an autophagic inducer, it has anti-cancer activity, it presents inhibitory effects on cancer cell lines tested(HepG2, MDA-MB-231, and MCF-7 cells).

Lucanthone hydrochloride is a novel acridine derivative which supresses autophagic degradation and triggers apoptosis in colon cancer cells.

NSC 185058, an inhibitor of ATG4B (a major cysteine protease), can also attenuate autophagic activity.

Aurantiamide has anti-cancer, anti-inflammatory and antinociceptive activities, it may suppress the growth of malignant gliomas by blocking autophagic flux.Aurantiamide has an anti-neuroinflammatory effect on LPS stimulation through its inhibition of the