MAGL-IN-5 is a non-selective lipase inhibitor with IC50 values of 144, 90, and 14 nM for human recombinant monoacylglycerol lipase(MAGL),hormone sensitive lipase(HSL), and fatty acid amide hydrolase(FAAH) respectively[1][2].
hnps-PLA-IN-1 (compound 5aa), a indole-3-acetamide, is a hnps-PLA2 inhibitor (IC50=0.124 μM)[1].
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study[1][2][3].
YTX-465 (YTX465) is a specific small molecule that rescues yeast from a-Syn cytotoxicity with EC50 of 15 nM, via inhibiting Ole1, the yeast homolog of human stearoyl-CoA desaturase (SCD); YTX-465 is inactive at SCD1.
Idraparinux (sodium) is a polymethylated synthetic pentasaccharide known to interact with the antithrombin III and act as anticoagulant.
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P4503A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults[1][2][3].
Acetazolamide D3 is deuterium labeled Acetazolamide, which is a potent carbonic anhydrase (CA) inhibitor.
Methazolamide is a carbonic anhydrase inhibitor used to treat glaucoma.Target: Carbonic AnhydraseMethazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively [1]. Methazolamide is of strength equal to acetazolamide, another carbonic anhydrase inhibitor used to treat irregular breathing disorders. However, methazolamide differs from acetazolamide in that it fails to activate Ca2+-dependent potassium channels in skeletal muscles. Methazolamide does not impair respiratory work performance in anesthetized rabbits [2]. Oral administration of methazolamide decreases IOPs and AHFRs in clinically normal dogs, with effectiveness diminishing in the evening [3].
Z-Arg-Arg-pNA is a substrate for cathepsin B and can be used to detect this enzyme activity[1].
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis[1][2][3].
ACC1/2-IN-1 (compound 4s) is a potent ACC1/2 inhibitor with IC50 values of 98.06 and 29.43 nM for ACC1 and ACC2, respectively. ACC1/2-IN-1 can be used for cancer research[1].
(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers[1].
Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research[1][2].
Kushenol A is isolated from the root of Sophora flavescent, a non-competitive tyrosinase inhibitor with IC50 and Ki values of 1.1 μM and 0.4 μM, respectively[1].Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase and beta-amylase[2].Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging[1].
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes[1].
AR7 is a retinoic acid receptor α (RARα) antagonist.
Baicalein 6-O-glucoside is a glucuronidation metabolite of Baicalein[1].
CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism[1].
ATX inhibitor 14 (compound 4), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 0.41 nM. ATX inhibitor 14 has the potential for fibrosis relevant diseases research[1].
Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications[1].
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1). IC50 value:Target: DAF-9(CYP27A1) inhibitorThe DAF-9 cytochrome P450 is a key regulator of dauer formation, developmental timing and longevity in the nematodeCaenorhabditis elegans. Here we describe the first identified chemical inhibitor of DAF-9 and the first reported small-molecule tool that robustly induces dauer formation in typical culture conditions. This molecule (called dafadine) also inhibits the mammalian ortholog of DAF-9(CYP27A1), suggesting that dafadine can be used to interrogate developmental control and longevity in other animals.
DPP-4-IN-1 (compound d1) is a potent DPP-4 (dipeptidyl peptidase 4) inhibitor, with an IC50of 49 nM. DPP-4-IN-1 is a structurally analogs of Alogliptin (HY-A0023A). DPP-4-IN-1 can be used for diabetes research[1].
Leucylarginylproline is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 0.27μM.
5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity.
Boc-QAR-pNA is a chromogenic substrate of trypsin. Boc-QAR-pNA can be used to test trypsin activity[1][2].
(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research[1].
Ikshusterol 3-O-glucoside is a phytochemical that inhibits PLA2 from snake venoms[1].
AHR-5333 is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity[1].
Asundexian (BAY 2433334) is an orally active coagulation factor Xia (FXIa) inhibitor. Asundexian binds directly, potently, and reversibly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC50 of 1 nM[1].
Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.