Zymostenol (5a-Cholest-8-en-3b-ol) is a late-stage precursor in the biosynthesis of cholesterol. Zymostenol is a RORγ agonist (EC50: 1 μM)[1][2][3].
MMP-9-IN-4 is a MMP-9 inhibitor (IC50: 7.46 nM) that has H-π interactions with MMP-9. MMP-9-IN-4 also inhibits AKT activity (IC50: 8.82 nM). MMP-9-IN-4 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-4 can be used in the research of cancers[1].
Broussoflavonol F possess xanthine oxidase inhibitory activity[1].
Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM[1].
Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with IC50 of 1.5 nM.
Lacto-N-fucopentaose III (LNFP-III) is an immune modulator. Lacto-N-fucopentaose III reduces the severity of experimental autoimmune encephalomyelitis (EAE) and CNS inflammation[1].
Efipladib is a potent, selective and orally active cPLA2α inhibitor with an IC50 of 0.04 μM and a Kd of 0.067 μM[1].
Epristeride is a novel 5α-reductase inhibor.
IDO1/TDO-IN-3 is a potent inhibitor of IDO1/TDO. IDO1/TDO-IN-3 exhibits significant activities against IDO1 (IC50: 0.005 μM) and TDO (IC50: 0.004 μM). IDO1/TDO-IN-3 shows considerable in vivo anti-tumor activity and no obvious toxicity is observed[1].
Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM[1].
4-Methylumbelliferyl phosphate (4-MUP) disodium, an anionic organophosphate, is a acid and alkaline phosphatase fluorogenic substrate. 4-Methylumbelliferyl phosphate disodium is also a nerve agent simulant[1][2][3].
FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain[1].
Moexipril-d5 is the deuterium labeled Moexipril. Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure[1][2].
Rev 5975 is a non-sulfhydryl ACE-inhibitor.
Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
HZ52 is a potent, reversible 5-lipoxygenase inhibitor, blocking leukotriene synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes[1].
AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2].
Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED), with less oral bioavailability than Lodenafil carbonate[1].
Arimoclomol maleate is a co-inducer of heat shock proteins (HSP).
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells[1]. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation[2].
MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs[1].
Ibudilast-d7-1 is the deuterium labeled Ibudilast[1]. Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[2].
Nequinate, a quinoline compound, is an anticoccidial agent against cecal coccidiosis (Eimeria tenella) infections[1]. Nequinate inhibits xanthine oxidoreductase (XOD) activity[2].
ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research[1].
Enpp-1-IN-9 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-9 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51)[1].
Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.
Pedalitin is a inhibitor of tyrosinase（IC50=0.28 mM） and α-glucosidase（IC50=0.29 mM）[1].
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for the treatment of inflammation related diseases[1].
Roxadustat (FG-4592) is an oral hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor developed for the treatment of anemia.