Pyrazinamide is a pyrazine that is used therapeutically as an antitubercular agent.Target: AntibacterialPyrazinamide is a prodrug that stops the growth of Mycobacterium tuberculosis. Pyrazinoic acid was thought to inhibit the enzyme fatty acid synthase (FAS) I, which is required by the bacterium to synthesise fatty acids although this has been discounted. It was also suggested that the accumulation of pyrazinoic acid disrupts membrane potential and interferes with energy production, necessary for survival of M. tuberculosis at an acidic site of infection. Pyrazinoic acid binds to the ribosomal protein S1 (RpsA) and inhibits trans-translation. This may explain the ability of the drug to kill dormant mycobacteria [1-4].
Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly more potent against BCR-ABL than Imatinib, and is active against many Imatinib-resistant BCR-ABL mutants.
Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor[1][2].
Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond.Target: Nucleoside antimetabolite/analogAdenosine plays an important role in biochemical processes, such as energy transfer — as adenosine triphosphate (ATP) and adenosine diphosphate (ADP) — as well as in signal transduction as cyclic adenosine monophosphate, cAMP. It is also an inhibitory neurotransmitter, believed to play a role in promoting sleep and suppressing arousal. Adenosine also plays a role in regulation of blood flow to various organs through vasodilation.Adenosine is an endogenous purine nucleoside that modulates many physiological processes. Cellular signaling by adenosine occurs through four known adenosine receptor subtypes. Extracellular adenosine concentrations from normal cells are approximately 300 nM; however, in response to cellular damage (e.g. in inflammatory or ischemic tissue), these concentrations are quickly elevated (600–1,200 nM). Thus, in regard to stress or injury, the function of adenosine is primarily that of cytoprotection preventing tissue damage during instances of hypoxia, ischemia, and seizure activity. Activation of A2A receptors produces a constellation of responses that in general can be classified as anti-inflammatory.
Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties.
SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
AZD 6482 is a potent and selective p110β inhibitor with IC50 of 0.69 nM.
Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
Flavopiridol is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is a autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria[2]. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis [1][2].
3,4-Dimethoxychalcone is a Caloric restriction mimetics (CRMs). 3,4-Dimethoxychalcone induces the deacetylation of cytoplasmic proteins and stimulates autophagy flux. 3,4-Dimethoxychalcone can be used for cardiac and cancer diseases research[1].
Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma[1][2][3][4][5].
Emetine (dihydrochloride) is an anti-protozoal drug previously used for intestinal and tissue amoebiasis[1].
Licochalcone A, a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch, presents obvious anti-cancer effects. The IC50 value is 0.97 μM for UGT1A1.
(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
(2-Hydroxypropyl)-β-cyclodextrin is a widely used drug delivery vehicle to improve the stability and bioavailability.
Dronedarone(Multaq) is a newer therapeutic agent with a structural resemblance to amiodarone and a better side effect profile; it is a multichannel blocker with antiadrenergic properties and has been evaluated in both rate and rhythm control strategies in the management of AF.IC50 value:Target: multichannel blocker
FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD+) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy[1][2].
Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
Dexmedetomidine Hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.Target: Adrenergic alpha-2 ReceptorDexmedetomidine, acting at alpha(2A) adrenoceptors, must be present during the encoding process to decrease discrete cue fear memory; however, its ability to suppress contextual memory is likely the result of blocking the consolidation process [1]. Dexmedetomidine had no analgesic effects in alpha(2A)-adrenoceptor KO mice [2]. Dexmedetomidine was effective in blocking these sympathomimetic actions of cocaine even in all 7 subjects who were homozygous for the Del322-325 polymorphism in the alpha2C AR, a loss-of-function mutation that is highly enriched in blacks [3].
(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine, a synthetic antimalarial drug, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker[1].
Nilotinib (AMN107) hydrochlorid is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2][3].
Aceglutamide is a psychostimulant and nootropic, used to improve memory and concentration.
RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.
MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities[1][2].
Nicardipine Hcl(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.