QW24 exerts potent anti-tumor activity by down-regulating BMI-1 and is used as an effective therapeutic agent for clinical colorectal cancer treatment.

SH498, a novel Bmi-1-mediated antitumor agent, shows potent antiproliferative activity.

SH379 is the derivative of 2-methylpyrimidine-fused tricyclic diterpene. SH379 is a potent and orally active anti-late-onset hypogonadism agent. SH379 significantly promotes the expression of the key testosterone synthesis-related enzymes StAR and 3β-HSD. SH379 stimulates autophagy through regulating AMPK/mTOR signaling pathway.

Mono-Pt is the first platinum(II) complex that inhibits cancer cells through a non-DNA-binding mitophagy pathway. Mono-Pt promotes the occurrence of mitophagy in cancer cells via stimulating endoplasmic reticulum stress (ERS) and activating unfolded protein response (UPR).

MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.

N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity.

ATG7-IN-1 is a potent and selective inhibitor of ATG7 (IC50 = 62 nM).

WH-4-025 is a Salt-inducible kinase (SIK) inhibitor (WO2016023014 A2).

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).

Autophagy-IN-C1 not only induces apoptosis but also blocks autophagy in hepatocellular carcinoma (HCC) cells.

Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).

cGMP-HTL contains a HT-ligand, a linker and the Cys-S-cGMP (autophagy tag). cGMP-HTL increases the K63-linked ubiquitination of mitochondria. AUTAC (autophagy-targeting chimera) is a novel targeted-clearance strategy that contains a degradation tag (guanine derivatives) and a warhead to provide target specificity.

MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC50 values of 516 nM, 180 nM and 127 nM for SIK1, SIK2 and SIK3, respectively.

Norswertianin, a xanthone compound, serves as a powerful anti-glioma compound. Norswertianin induces GBM cells differentiation through oxidative stress and Akt/mTOR dependent autophagy.

CZC-54252 hydrochloride is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 hydrochloride with an EC50 of ~1 nM.CZC-54252 hydrochloride has a neuroprotective activity.

AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC4 downregulates cytosolic proteins and promots targeted mitochondrial turnover via mitophagy.

Olaparib D4 (AZD2281 D4) is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.

Clematichinenoside AR is a major active ingredient that could be extracted from the traditional Chinese herb Clematis chinensis and has potent pharmacological effects on various diseases, including atherosclerosis (AS).

Corynoxine hydrochloride, a tetracyclic oxindole alkaloid, is isolated from the hooks of Uncaria macrophylla. Corynoxine hydrochloride is a natural autophagy enhancer that promotes the clearance of alpha-synuclein via Akt/mTOR pathway.

Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).

Sedanolide, a natural compound occurring in edible umbelliferous plants, possesses anti-inflammatory and antioxidant activities.

(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM.

Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.

(3S,5R)-Fluvastatin D6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive?HMG-CoA reductase?inhibitor with an IC50?of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.

Zingiberene (α-Zingiberene) is a monocyclic sesquiterpene which is the predominant constituent of ginger with oil content (Zingiber officinale). Neuroprotective potential. Zingiberene triggers autophagy. Anticancer activity.

THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.

AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG (p-Fluorobenzyl Guanine) and an SLF (c ligand of FKBP) moiety. SLF binds non-covalently to FKBP12.

AUTAC1 is a MetAP2-targeting autophagy-mediated degrader (AUTAC). AUTACs contain a degradation tag and a warhead to provide target specificity. AUTAC1 contains an FBnG (p-Fluorobenzyl Guanine) and a Fumagillol moiety. Fumagillol binds covalently to MetAP2.

EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.

Cearoin, isolated from Dalbergia odorifera, increases autophagy and apoptosis through the production of ROS and the activation of ERK.