Other inhibitors

Ethotoin is an anticonvulsant drug used in the treatment of epilepsy. It is a hydantoin, similar to phenytoin. Ethotoin lacks phenytoin's side effects of gingival hyperplasia and hirsutism; however, it is less effective. This, combined with the need for frequent dosing has limited its usefulness. Ethotoin is no longer widely used.

Haloperidol decanoate is a typical antipsychotic drug used as maintenance therapy for schizophrenia and mood disorders formulated as an ester for intramuscular injection.

Hydroflumethiazide is a thiazide diuretic that also inhibits carbonic anhydrase (CA). It is selective for CAII, VB, VII, IX, XII, and XIV (Kis = 305-235 nM) over CAI, IV, and VI (Kis = 2,840-8,250 nM) and CAIII, VA, and XIII (Kis = >10 ?M).

Timonacic is a cyclic sulfur amino acid derivative with potential antineoplastic and antioxidant activities.

Bismuth subcitrate contains tripotassium di-citratobismuthate used in gastric & duodenal ulcer therapy. Bismuth subcitrate potassium is a bismuth salt used in combination with antibiotics and a proton pump inhibitor for the treatment of Helicobacter pylori infections.

Hydrocortisone buteprate (Hydrocortisone probutate) is a medium potent, non-halogenated double-ester of hydrocortisone with a favorable benefit/risk ratio for the treatment of inflammatory skin disorders.

Metixene hydrochloride hydrate is an anticholinergic antiparkinsonian agent, potently inhibits binding of quinuclidinyl benzilate (QNB) to the muscarinic receptor in rat brain cortical tissue, with an IC50 of 55 nM and a Kd of 15 nM.

Tolazamide is an oral blood glucose lowering drug used for people with Type 2 diabetes. It is part of the sulfonylurea family (ATC A10BB).

Oxalamine Citrate is a cough suppressant.

Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.

Ethamivan, or etamivan, is a respiratory stimulant drug related to nikethamide. It has been mainly used in the treatment of barbiturate overdose and chronic obstructive pulmonary disease.

Heptaminol hydrochloride is an amino alcohol used as a myocardial stimulant, vasodilator, and to relieve bronchospasm. Its most common therapeutic use is in orthostatic hypotension.

Sulfacarbamide is an antimicrobial agent that has been investigated as a therapeutic biochemical for diabetes treatment. It may lower blood sugar.

Quinidine is a dextrorotatory stereoisomer of quinine with antimalarial and antiarrhythmic properties.

Fursultiamine is a compound used for therapy of thiamine deficiency. It??s phosphorylated metabolites may be administered as multivitamin preparations. Fursultiamine has been identified as a drug candidate against prostate cancer from the aspect of somatic cell reprogramming and may be useful as a therapeutic tool in number of human neurological diseases.

Apronalide, also known as Allylisopropylacetylurea or Apronal, is a hypnotic/sedative drug of the ureide (acylurea) group which may induce cytochrome P-450 through barbiturate-like activity.

Triamcinolone hexacetonide is an anti-inflammatory.

Cholestyramine (Colestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.

Calcium polystyrene sulfonate is an ion-exchange resin used for reducing blood levels of potassium. Calcium polystyrene sulfonate is used to treat hyperkalemia in patients with chronic kidney disease (CKD).

Talaporfin (ME2906; NPe6) is a photosensitizer used in photodynamic therapy (PDT).

PF-3187207 is a a nitric oxide (NO)-donating latanoprost with prostaglandin activity. It loweres intraocular pressure (IOP) more effectively than latanoprost in monkeys, dogs and rabbits.

Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities. Upon administration, polaprezinc increases the expression of various anti-oxidant enzymes, such as superoxide dismutase 1 (SOD-1), SOD-2, heme oxygenase-1 (HO-1), glutathione S-transferase (GST), glutathione peroxidase (GSH-px), peroxidredoxin-1 (PRDX1; PRXI) and PRXD5 (PRXV) in the gastric mucosa, which protect cells against reactive oxygen species (ROS).

Flurandrenolide is a synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Flurandrenolide exerts its effects by interacting with specific cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression.

Vinburnine, also known as Eburnamonine, is a vasodilator. Vinburnine is a vinca alkaloid and a metabolite of vincamine.

Dodecyl alcohol, ethoxylated is a bioactive chemical.

Famprofazone, also known as Geodowin, is an analgesic used for fever and pain relief. Famprofazone has been demonstrated to be metabolized to methamphetamine and amphetamine following administration. Data shows the famprofazone metabolites amphetamine and methamphetamine to be both d- and l-enantiomers.

Lofendazam is a benzodiazepine derivative that has sedative and anxiolytic effects.

KL-1 is an inhibitor of SEC and transcription elongation by Pol II which disrupts the cyclin T1-AFF4 interaction within SEC, and attenuates SEC-dependent rapid transcriptional responses. KL-1 inhibits MYC transcriptional programs.

EC1454 is an anti-tumor compound, extracted from US20170348376A1.

Thiamine diphosphate analog 1 is an analog of Thiamine diphosphate. Thiamine diphosphate is the active form of vitamin B1. Thiamine diphosphate a universal cofactor involved in pivotal cellular pathways.

SKF-34288 hydrochloride (3-Mercaptopicolinic acid) is a phosphoenolpyruvate carboxykinase (PEPCK) inhibitor. SKF-34288 hydrochloride is a potent hypoglycemic agent via inhibition of glucose synthesis through the specific inhibition of PEPCK in the gluconeogenesis pathway.

MT-4 blocks the TG2/FN complex at the interface between cancer cells and the tumor niche. MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.

ITIC, non-fullerene acceptor, is an indacenodithienothiophene-based postfullerene electron acceptor, crystallizes in a profoundly different way as compared to fullerenes. ITIC has a superior thermal stability and undergoes a glass-crystal transition considerably below its high Tg of 180 ??C.

NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor, binds to the conserved Leu-90 of NAC1, prevents its homodimerization, and leads to proteasomal NAC1 degradation. Anti-cancer activity.

DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.

Kgp-IN-1 is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R.

Eperisone is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. Eperisone is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect.

TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.

SPL-410 is an orally active, highly potent and selective hydroxyethylamine based SPPL2a (Signal Peptide Peptidase Like 2a) inhibitor, with an IC50 of 9 nM.

DPA-714 is a selective ligand for the translocator protein (TSPO) currently under evaluation for several clinical applications.It is also a PET tracer binding the TSPO receptor and highly expressed in myeloid cells.

Zylofuramine is a psychomotor stimulant.

ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.

BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.

BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM.

Dicyclanil is an insect growth regulator compound with a similar chemical structure to cyromazine.

D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity.

AKOS B018304 is an arylalkylidene derivative, with polar substitution at para-position.

Ly93 is a selective and oral active sphingomyelin synthase 2 (SMS2) inhibitor, with an IC50 of 91 nM.

ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats.

(S)-Metolachor, a derivative of aniline, is a major pesticide in use.