Autophagy Inhibitor

Methyllycaconitine (MLA) citrate is a blood-brain barrier-permeable antagonist of α7 nicotinic acetylcholine receptor (α7nAChR) with an IC₅₀ of 2 nM. Methyllycaconitine citrate inhibits Aβ_25-35-induced autophagy by restoring the mTOR pathway, and prevents reactive oxygen species (ROS) production, microglial activation, reduced dopamine uptake, loss of dopaminergic terminals and catecholamine secretion. Methyllycaconitine citrate induces hippocampal glutamate efflux, enhances long-term potentiation, and improves memory acquisition. Methyllycaconitine citrate can be used in research related to Alzheimer's disease, cerebral palsy, Parkinson's disease and schizophrenia.

U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC₅₀=1.2 nM; K_d=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.

GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC₅₀ of 0.9 nM.

LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with K_is of 38 nM and 300 nM, respectively.

Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC₅₀s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

Azithromycin is a macrolide antibiotic useful for the treatment of a number of bacterial infections.

Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.

Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC₅₀s of 0.6-0.7 μM.

TWS119 is an inhibitor of GSK-3β, with an IC₅₀ of 30 nM, and activates the wnt/β-catenin pathway.

MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC₅₀s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC₅₀s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.

Heparin sodium salt (MW 15kDa) (Sodium heparin (MW 15kDa)) is a polymer of Heparin with the molecular weight of 15kDa. Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.

Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC₅₀ value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.

Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS).

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC₅₀s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD⁺ and NADH. 3PO can be used for the research of cancer.

6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.