reversible

Avibactam sodium (NXL-104) is a reversible β-lactamase inhibitor (IC50: 8 80 38 nM, for TEM-1 P99 KPC-2 β-lactamases).

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

TVB-3664 significantly decreases tubulin palmitoylation and mRNA expression. TVB-3664 is a reversible and highly bioavailable fatty acid synthase inhibitor (IC50: 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively).

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

MG-132 (Z-Leu-Leu-Leu-al) is a cell-permeable, reversible 26S proteasome inhibitor (IC50=100 nM) that functions as an autophagy activator and induces apoptosis.

SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40/40/90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

Foscarnet sodium (Phosphonoformate) is an antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.

Neostigmine methyl sulfate (Syntostigmin) is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier, used in the treatment of myasthenia gravis.

Nizatidine (Acinon) is a competitive and reversible histamine H2-receptor antagonist with antacid activity.

Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).

Donepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type.

Indobufen (Ibustrin) is an inhibitor of platelet aggregation and is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.

4-Diethylaminobenzaldehyde, a reversible aldehyde dehydrogenase (ALDH) inhibitor (Ki: 4 nM for ALDH1), exhibits a potent anti-androgenic effect (IC50: 1.71 μM).

Eprosartan Mesylate (SKF-108566J) is a competitive and reversible Angiotensin II Receptor Blocker.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Deltamethrin (RU 22974), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis.Deltamethrin is globally used in crop protection, control of malaria and other vector-borne diseases. It is easily degradable.

Purpurin (Verantin) was a reversible and competitive inhibitor of MAO-A with a Ki value of 0.422μM. it exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities.

Carbaryl (1-naphthyl methylcarbamate) is a carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries.

Ranitidine Hydrochloride (AH19065) is a member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. In addition, other substances that promote acid secretion have a reduced effect on parietal cells when the H2 receptors are blocked.

Isovanillin (5-Formylguaiacol) is a reversible inhibitor of aldehyde oxidase. It is largely used as pharmaceutical intermediates and also applied in food and beverage industry, synthetic fragrances, chemical.

Bupivacaine hydrochloride (Vivacaine) is a long-acting, amide-type local anesthetic. Bupivacaine hydrochloride reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation.

Gimeracil (Gimestat) is a competitive, reversible inhibitor of dihydropyrimidine dehydrogenase.

Benzamidine hydrochloride (Benzamidine HCl) is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Ki of 35, 350, and 220 μM, respectively).

RS 61443 (Mycophenolate mofetil) is an immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH)

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor and the pure S(-)-enantiomer of bupivacaine, used as a long-acting local anesthetic.

Benzylacetone (4-Phenyl-2-butanone) is an aromatic compound extracted from incense wood. Benzylacetone has appetite-enhancing and exercise-reducing properties. Benzylacetone has a strong and reversible anti-mushroom tyrosinase effect, with IC50 values of 2.8 mM and 0.6 mM for monophenolase and biphenolase effects, respectively.

Entacapone (OR-611) is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT).

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive, and orally active pan-PTP (protein tyrosine phosphatases) inhibitor with insulin-mimicking effects and anti-diabetic properties. BMOV is a potent insulin sensitizer and has been shown to improve cardiac dysfunctions in diabetic models. BMOV inhibits HCPTPA, PTP1B, HPTPβ, and SHP2 with IC50s of 126 nM, 109 nM, 26 nM, and 201 nM, respectively [1][2].

Finrozole (MPV 2213ad) is a novel selective aromatase inhibitor that is partially reversible for breast development.

hMAO-B-IN-5 is a potent reversible and selective human monoamine oxidase hMAO-B inhibitor (IC50:0.12μM). hMAO-B-IN-5 can cross the blood-brain barrier and can be used in the study of Parkinson's disease. It is a promising compound in the treatment and diagnosis of central nervous system diseases.

Acetyl-Calpastatin (184-210)(human) acetate is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.

hPL-IN-1 is a potent reversible pancreatic lipase (PL) inhibitor (IC50=1.86 μM) that can be used to study obesity-related diseases.

AChE BChE MAO-B-IN-1 is a reversible, non-time-dependent inhibitor of AChE, BChE, and MAO-B that crosses the blood-brain barrier, exhibiting inhibitory effects on hAChE, hBChE, and hMAO-B with IC50s of 7.31, 0.56, and 26.1 μM, respectively. [AChE BChE MAO-B-IN-1] had a neuroprotective effect and was not significantly cytotoxic.

Esuprone (LU-43839) is a novel reversible and highly selective MAO-A inhibitor with anticonvulsant activity for the treatment of depression.

A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16 46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th

AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively).

CHBO4 is an hMAO-B inhibitor that is potent, reversible, competitive and selective.The IC50 value of CHBO4 against hMAO-B in the CHBO assay was 0.031 μM, and the Ki value was 0.010 ± 0.005 μM.CHBO4 reduces cellular damage by scavenging intracellular reactive oxygen species (ROS), and can be used to study Parkinson's disease (PD).

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activity.CBS9106 inhibits CRM1-dependent nuclear export and reduces CRM1 protein levels.CBS9106 inhibits tumor growth and prolongs the survival of mice bearing tumor xenografts.CBS9106 is an inhibitor of CRM1-dependent nuclear export and reduces CRM1 protein levels.

BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

Ticagrelor metabolite M5 (T437700) is a metabolite of Ticagrelor, the first reversible oral antagonist of P2Y12 receptor. Compared to Clopidogrel, Ticagrelor has faster and more consistent inhibition on ADP-receptors. Ticagrelor is used in the treatment of acute coronary syndromes (ACS).

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

ND-011992 is a reversible and selective quinazoline inhibitor targeting quinone reductases and quinol oxidases.ND-011992 inhibits E. coli BL21*Δcyo respiratory complex I. ND-011992 inhibits bo3 oxidase, bd-I oxidases and bd-II oxidases, ND-011992 inhibits E. coli BL21*Δcyo respiratory complex I, bo3 oxidase, bd-I oxidases, and bd-II oxidases with IC50s of 0.12, 2.47, 0.63, and 1.3 μM, respectively.ND-011992 can be used in the study of tuberculosis.

Bazinaprine is a selective, reversible monoamine oxidase inhibitor (MAOI) that is a candidate compound for the treatment of depression. Bazinaprine showed strong inhibitory effect on type A monoamine oxidase and weak inhibitory effect on type b monoamine oxidase. Bazinaprine is reversible in vivo, but not in vitro.

Entacapone acid (AG 1290) is a selective and reversible inhibitor of catechol-O-methyltransferase(COMT).

Clozic (ICI 55897) exhibits reversible anti-proliferative effects and can be used in studies about serving as a potential anti-arthritic agent.

rac-CCT-250863 HCl is a selective and reversible inhibitor of NEK 2. rac-CCT-250863 HCl induces cell cycle arrest and has good anti-proliferative activity against cancer cells. rac-CCT-250863 HCl can be used in combination with Pomalidomide to induce apoptosis and can be used in combined anti-cancer studies.

UNC 569 hydrochloride is a reversible and ATP-competitive inhibitor of Mer with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC 569 hydrochloride inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC 569 hydrochloride can be used in studies about acute lymphoblastic leukemia and atypical teratoid/rhabdoid tumors.