VU0285655-1 is a potent, selective inhibitor of PLD2, induces autophagy in colorectal cancer cells

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.

MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease.

NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.

hDHODH-IN-8 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 16 nM. hDHODH-IN-8 has potent antiproliferative activity and excellent aqueous solubility. hDHODH-IN-8 has the potential for the research of tumor disease, especially lymphoma.

Z-Arg-Lys-AOMK is a potent, selective, irreversible neutral pH 7.2 inhibitor of Cathepsin B with IC50 of 13 nM, >100-fold higher potent than at pH 4.6 (IC50=1,830 nM). Z-Arg-Lys-AOMK displayed high specificity for cathepsin B compared to other lysosomal cysteine cathepsins. Z-Arg-Lys-AOMK selectively inhibits cathepsin B cleavage of peptides at neutral cytosolic pH compared to acidic lysosomal pH conditions. Z-Arg-Lys-AOMK completely inhibited cathepsin B in human neuroblastoma cell lysates at 1 uM. Z-Arg-Lys-AOMK is cell permeable and inhibits intracellular cathepsin B.

ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.

Zagociguat is the stimulator of soluble guanylate cyclase. Zagociguat increases nitric oxide (NO) signaling leading to an increase in cyclic guanosine monophosphate production. Zagociguat has the potential for the research of noncentral nervous system (CNS) disorders.

MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.

NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression.

1,3-Butanediol, an ethanol dimer providing a source of calories for human nutrition. 1,3-Butanediol is converted in the body to β-hydroxybutyrate and has cerebral protective and hypoglycaemic effect.

L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia.

NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 bind

MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2.

AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1. AD-5591 (100  μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins. AD-5591 is the active form of AD-9308.

AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591.

GCPII-IN-1 TFA is a glutamate carboxypeptidase II (GCPII, or PSMA) inhibitor scaffold with a Ki of 44.3 nM.

Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM.

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

GSK-484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.

GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively.

AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate.

MK-3102 (MSD) is a novel DPP-4 Inhibitor, which improves glycaemic control with low risk of symptomatic hypoglycaemia.

ZED3197 (ZED-3197) is a novel peptidomimetic direct-acting, potent and selective inhibitor of human FXIIIa, inhibits human plasma derived FXIII‐A2B2 and the recombinant cellular form (FXIII‐A2) with IC50 of 10 and 14 nM, respectively.ZED3197 strongly blocks FXIII‐A2 from mouse, rat, rabbit, dog, and cynomolgus monkey (IC50 8-30 nM), is a significantly weaker inhibitor of FXIII‐A2 from pig (IC50=220 nM).ZED3197 displays 20‐fold to 3000‐fold selectivity against human transglutaminases TG1, TG2, TG3, and TG7.ZED3197 prolonged clot formation, reduced clot firmness, and facilitated clot lysis in whole human blood without affecting the clotting time, indicating minimal impact on hemostasis.ZED3197 effectively decreased the weight of clots and facilitated flow restoration without prolongation of the bleeding time in vivo.

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM.

(+)-Narwedine. Galantamine(Narwedin) is a competitive and reversible cholinesterase(AChE) inhibitor.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.