RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC)[1][2][3][4].
Melagatran is a direct and oral active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia[1]. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion[2].
IDH2R140Q-IN-2 (compound 36) is an an orally active IDH2R140Q inhibitor (IC50: 29 nM). IDH2R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2R140Q (IC50: 10 nM). IDH2R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2R140Q-IN-2 can be used for research of acute myeloid leukemia (AML)[1].
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ[1][2].
Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin and cholesterol ester transfer protein[1][2][3].
5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitory activities[1].
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
Glycolic Acid is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively[1].
Edaravone D5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect[1][2].
LAS-31180 is an inhibitor of phosphodiesterase 3, with positive inotropic and vasodilator properties.
Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor for the treatment of osteoarthritis. Licofelone (ML-3000) exerts anti-inflammatory and anti-proliferative effects. Licofelone (ML-3000) induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[1][2].
AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50 of 190±8.1 nM.
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively[1].
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate for and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant[1].
Nampt-IN-10 TFA (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 TFA shows cellular potency to A2780 and CORL23 cells lines with IC50s of 5 and 19 nM, respectively. Nampt-IN-10 TFA can be used as a novel non-antimitotic payload for ADCs[1].
SZL P1-41 is Skp2 inhibitor, selectively suppresses Skp2 E3 ligase activity, but not activity of other SCF complexes.target: Skp2In vitro: SZL P1-41 also phenocopies the effects observed upon genetic Skp2 deficiency, such as suppressing survival, Akt-mediated glycolysis as well as triggering p53-independent cellular senescence. SZL P1-41 prevent Skp2-Skp1 interactions and Skp2 SCF E3 ligase activity. The reference concentration is 5 uM. SZL P1-41 restricts cancer cell survival through triggering p53-independent cellular senescence and inhibiting aerobic glycolysis.In vivo: SZL P1-41 exhibits potent anti-tumor activities in multiple animal models and cooperates with chemotherapeutic agents to reduce cancer cell survival.
Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1 (PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer[1].
MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
Danoprevir is a NS3/4A protease inhibitor for hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM. The inhibition effect on HCV genotypes 1A/1B/4/5/6 is approximately 10-fold higher than 2B/3A.
PCSK9-IN-1 is a novel and highly potent cyclic peptide PCSK9 inhibitor with a Ki value of 1.46 nM.
4'-Methoxyisoagarotetrol is chromone derivative and shows moderate PDE?3A inhibitory activity (IC50=54 μM)[1].
PCSK9-IN-16 is a potent PCSK9 inhibitor. PCSK9-IN-16 is extracted from patent WO2020150474, example 87, has the potential for hypercholesterolemia and other cardiovascular diseases research[1].
Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT)[1].
hCAI/II-IN-6 is a human carbonic anhydrase(CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy[1].
PDE4B-IN-2 is an orally active and selective PDE4B inhibitor (IC50=15 nM) and exhibits >100-fold selectivity for PDE4B over 4D. PDE4B-IN-2 regulates cAMP in inflammatory cells and inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. PDE4B-IN-2 reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. PDE4B-IN-2 also exhibits antidepressant-like effects.
LP117 is a novel and potent inhibitor of 5-Lipoxygenase (5-LO) product synthesis with an IC50 of 1.1 μM.