LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Mupirocin calcium hydrate is an antibiotic produced by Pseudomonas fluorescens, showed a high level of activity against staphylococci and streptococci and against certain gram-negative bacteria

Procainamide Hydrochloride (Procapan) is the hydrochloride salt form of procainamide, an amide derivative exhibiting class 1A antiarrhythmic property and analog of procaine. Procainamide hydrochloride reversibly binds to and blocks activated (open) voltage-gated sodium channels, thereby blocks the influx of sodium ions into the cell, which leads to an increase in threshold for excitation and inhibit depolarization during phase 0 of the action potential.

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

Sodium 4-phenylbutyrate (TriButyrate), a transcriptional regulator, reversibly inhibits class I and II histone deacetylases (HDACs )resulting in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations.

Heparin sodium is a sulfated polysaccharide, which belongs to the family of glycosaminoglycans. It is utilized as an anticoagulant and interacted with diverse proteins for numerous important biological activities.Heparin sodium salt (Sodium heparinate) significantly inhibits exosome-cell interactions.

HC-067047 hydrochloride is a potent and selective TRPV4 antagonist. HC-067047 hydrochloride reversibly inhibited currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 486 nM, 133nM, and 17 nM, respectively.

10Panx Acetate is a mimetic inhibitory peptide that readily and reversibly inhibits the panx1 currents.

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

Dynasore (Dynamin Inhibitor I), a cell-permeable chemical, can reversibly and non-competitivity inhibit GTPase activity of dynamin 1/2 (IC50: 15 μM in a cell-free assay). It also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase.

DIDS, an anion exchange inhibitor, acts by blocking reversibly and later irreversibly, exchangers such as chloride-bicarbonate exchanger. It is also a RAD51 inhibitor.

Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR than PDGFRβ, lack of activity against InsR, EGFR, and FGFR. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature.

Pravastatin is a lipoprotein-lowering drug via reversibly inhibiting hydroxymethylglutaryl-CoA (HMG-CoA) reductase and the synthesis of very-low-density lipoproteins.

Cardanol triene is a phenol found in cashew nut shell liquid that reversibly inhibits tyrosinase with an IC50 value of 40.5 μM in vitro. A mixture of cardanol mono-, di-, and triene is used to synthesize cardanol-metal complexes that inhibit uropathogenic E. coli biofilm formation.

DL-Glyceraldehyde-3-phosphate (GADP) is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. In glycolysis, it can be derived from fructose 1,6-bisphosphate by fructose bisphosphate aldolase in a reaction that also produces dihydroxyacetone phosphate (DHAP). Triose phosphate isomerase reversibly converts DHAP to GADP. GADP is processed to 1,3-bisphosphoglycerate by glyceraldehyde phosphate dehydrogenase and NAD+.

Selective CaV3.1 channel blocker (IC50 values are 0.2 and 31.8 μM for hCaV3.1 and hCaV3.2 respectively). Also reversibly inhibits NaV1.8 and blocks KV2.1 channels.

Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversibly converted to phosphatidylethanolamine by phosphatidylserine decarboxylase in the mitochondria. Phosphatidylserine binds to T cell immunoglobulin mucin type 1 (TIM-1) and TIM-4 receptors as well as brain-specific angiogenesis inhibitor 1 (BAI1), leading to anti-inflammatory and anti-atherosclerotic effects. It is also a cofactor involved in the activation of various signaling pathways through activation of protein kinase C, neutral sphingomyelinase, and c-Raf-1 protein kinase among others. Phosphatidylserine is externalized during apoptosis by scramblases in the plasma membrane as a signal for phagocytes to engulf the cell. Phosphatidylserines (bovine) is a mixture of bovine phosphatidylserines containing fatty acids with variable chain lengths at the sn-1 and sn-2 positions.

Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum (ER) and can be reversibly converted back by the same enzymes. It can also be irreversibly converted to phosphatidylethanolamine by phosphatidylserine decarboxylase in the mitochondria. Phosphatidylserine binds to T cell immunoglobulin mucin type 1 (TIM-1) and TIM-4 receptors as well as brain-specific angiogenesis inhibitor 1 (BAI1), leading to anti-inflammatory and anti-atherosclerotic effects. It is also a cofactor involved in the activation of various signaling pathways through activation of protein kinase C, neutral sphingomyelinase, and c-Raf-1 protein kinase among others. Phosphatidylserine is externalized during apoptosis by scramblases in the plasma membrane as a signal for phagocytes to engulf the cell. Phosphatidylserines (soy) is a mixture of soy phosphatidylserines containing fatty acids with variable chain lengths at the sn-1 and sn-2 positions.

PR 39 (porcine) acetate is a noncompetitive, reversible and allosteric proteasome inhibitor. PR 39 (porcine) acetate reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway.

Asundexian (BAY-2433334) is a potent and orally active inhibitor of the coagulation factor FXIa that directly and reversibly binds to the active site of FXIa, thereby inhibiting its activity.Asundexian has an IC50 of 1 nM for human FXIa in buffer.Asundexian has antitumor activity and may be useful in studies of Acute ischemic stroke, transient ischemic attack and ischemic stroke.

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membranes, blocking activation.[2] PKC inhibitor peptide is commonly used in cells to evaluate the role of PKC in various cellular responses.[3],[4],[5]

α-Pompilidotoxin (α-PMTX), a neurotoxin sourced from Anoplius samanensis venom, reversibly and dose-dependently enhances excitatory postsynaptic currents (EPSCs), serving as a valuable tool in neuroscience research [1].

Streptolysin O causes both lysis of cells and cardiotoxicity. Streptolysin O is widely used for the controlled permeabilization of cell membranes. Streptolysin O exists in two forms, a reduced active state and an oxidized reversibly inactive state .

Peptide neurotoxin; selectively and reversibly blocks N-type calcium channels (IC50 = 0.15 nM). Reduces (RS)-3,5-DHPG -induced long term depression in vivo.

Methiocarb, a carbamate pesticide, is used as an insecticide, acaricide, bird repellent, and molluscicide. Methiocarb stimulates cholinergic by inhibiting reversibly acetylcholinesterase activity, making methiocarb a potent neurotoxin.

PZ-1922 (Compound 16), able to cross the blood-brain barrier, is a dual antagonist for 5-HT6R and 5-HT3R with K i values of 17 nM and 0.45 nM, respectively. It also reversibly inhibits MAO-B with a pIC50 of 8.93. Moreover, PZ-1922 mitigates scopolamine (SCOP)-induced memory deficits in rats as observed in the novel object recognition (NOR) test and hinders Aβ-induced memory impairment in the T-maze test [1].

Milvexian (BMS-986177) is a potent antithrombotic compound that inhibits human and rabbit factor XIa (FXIa) directly and reversibly. It is orally-bioavailable and exhibits a K i of 0.11 nM and 0.38 nM against human and rabbit FXIa, respectively.

Trichostatin C is a glycosylated derivative of trichostatin A , the antifungal antibiotic that reversibly inhibits histone deacetylase. Trichostatin C is reported to be the first example of a glucopyranosyl hydroxamate identified in nature. It has been shown to induce the differentiation of a mouse erythroleukemia cell line and to increase histone H4 acetylation in B cells, though at higher concentrations than trichostatin A.

Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

Cudratricusxanthone A has potent anti-proliferative, antioxidative, and monoamine oxidase inhibitory effects, it also possesses anti-cancer activities and provide a basis for developing effective therapeutic agents to inhibit growth and metastasis of brea

Ropivacaine mesylate, a long-acting amide local anaesthetic, is used for spinal block and effectively mitigates neuropathic pain. It achieves analgesia by reversibly inhibiting sodium ion influx in nerve fibers, thus blocking impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes.

p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine HCL) is a novel, potent and specific inhibitor of TPH[1]. The potential for p-Ethynylphenylalanine hydrochloride to inhibit selectively and reversibly the biosynthesis of serotonin may contribute to the characterization of the role of serotonin in behavioral and physiological activities[1].

Revaprazan is a novel, selective potassium-competitive acid blocker, to be specific, it reversibly inhibits gastric H(+)/K(+)-ATPase and shows effective acid suppression comparable to PPIs.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell/basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Vanillin (Zimco) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine.Vanillin can reversibly and non-competitively inhibit the cellulase activity at appropriate concentrations and the value of IC50 was estimated to be 30 g/L.Vanillin protects KSC from UVB irradiation and its effects may occur through the suppression of downstream step of MDM2 in UVB irradiation-induced p53 activation. Vanillin also inhibits yeast growth and fermentation.

Fabomotizole hydrochloride (CM346 hydrochloride), an anxiolytic drug, produces anxiolytic and neuroprotective effects. The mechanism of Afobazole remains poorly defined, however, with GABAergic, NGF, and BDNF release promoting, MT1 receptor antagonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Afobazole inhibits MAO-A reversibly and there might be also some involvement with serotonin receptors.

Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

Ambenonium chloride tetrahydrate is a salt of ambenonium --- a quaternary ammonium compound with parasympathomimetic activity. It is a cholinesterase inhibitor used in the management of myasthenia gravis. Myasthenia gravis occurs when the body produces antibodies against acetylcholine receptors, and thus inhibits signal transmission across the myoneural junction. Ambenonium chloride is a rapid indirect-acting cholinergic agonist that reversibly blocks the activity of acetylcholinesterase, thereby prevents acetylcholine hydrolysis and prolonging its activity on nicotinic receptors at the neuromuscular junction.

Optovin is a TRPA1 activator, which is reversibly photoactivated.

Articaine (Hoe-045 free base), an amide anesthetic featuring an ester group, effectively relieves pain by reversibly binding to the α-subunit of the voltage-gated sodium channels located in the nerve's inner cavity. Furthermore, Articaine mitigates LPS-induced acute kidney injury through the suppression of NF-κB activation and inhibition of the NLRP3 inflammasome pathway.

QM295 is a selective, reversibly reactive thiol inhibitor of endoplasmic reticulum oxidation 1 (ERO1), utilized in research related to endoplasmic reticulum stress.

Afegostat is a pharmacological chaperone that specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum with high affinity.

Fluphenazine is a traditional antipsychotic compound that tightly binds the dopamine D2 receptor (Ki = 0.55 nM) and also reversibly inhibits calmodulin at micromolar concentrations. Fluphenazine-N-2-chloroethane is a derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding. It is a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo, inactivating approximately 90% of D2 receptors in mice within 4 hours of treatment. Through this action, fluphenazine-B-2-chloroethane can be used to induce catalepsy in mice. It irreversibly inhibits calmodulin at higher doses (IC50 = 10 μM), which can sensitize cancer cells to TRAIL-induced apoptosis.

AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal preparation, AT-1001 inhibits nicotine-induced [³H]dopamine release poorly and at significantly higher concentrations compared with mecamylamine and conotoxin MII.

Sancycline (Bonomycin) is a rare semi-synthetic tetracycline, acts by reversibly binding to the 30S ribosomal subunit and inhibiting protein translation by blocking entry of aminoacyl-tRNA into the ribosome A site.

PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P (IC50 of 175 nM).

Trilostane (Win 24540) is a synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex.