Transferase

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor (EC50 of 3 μM in cells) that can be used to study OGT inhibition in different human cell lines.

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

OGT inhibitor 4a is an O-linked n-acetylglucosaminyltransferase (OGT) inhibitor with anticancer activity for the study of autoimmune and neurological disorders.

Serotonin (5-hydroxytryptamine) is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin regulates the nervous system, digestive system and cardiovascular system.

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor with potential anti-inflammatory activity. It mitigates statin-induced toxicity in human skeletal muscle cells and protects guinea pigs from simvastatin-induced myotoxicity, useful for research on hypercholesterolemia and HMG-CoA reductase deficiency.

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).

Glycosyltransferase-IN-1 is a glycosyltransferase inhibitor with bacteriostatic activity, inhibiting MSSA, MRSA, Bacillus subtilis, and Enterobacteriaceae.

PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2.

UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a nucleotide sugar synthesized from glucose through the hexosamine biosynthetic pathway (HBP).

Benzyl-α-GalNAc (O-glycosylation-IN-1) is a potent inhibitor of O-glycosylation and is used to reduce mucin on cell surfaces.

A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

SGN-2FF is an oral fucosylation inhibitor and inhibits fucosyltransferase activity, and has antitumor activity.

Eliglustat (Genz 99067) is an oral inhibitor of glucosylceramide synthase which is used in the therapy of type 1 Gaucher disease.

OSMI-3 is a potent and cell-permeable inhibitor of O-GlcNAc transferase (OGT) for the study of cancer and cardiovascular disease.

Ibiglustat (GZ402671) is a potent and selective Glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor. Ibiglustat blocks the formation of glucosylceramide (GL-1), a key intermediate in the synthesis of GL-3. Ibiglustat is potentially useful for treating Fabry disease. Fabry disease is a rare lysosomal storage disorder, which results in abnormal tissue deposits of a particular fatty substance called globotriaosylceramide (GL-3 or Gb3) throughout the body.

L-739750 2HCl is a potent inhibitor of peptidomimetic farnesyltransferase, a novel pseudopeptide mimetic with potential anticancer activity.

Miglustat (NB-DNJ) is an alkylated product of imino sugar deoxynojirimycin.It is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).

Rosmarinic acid (Labiatenic acid) is widely found in plants and has antioxidant, anti-inflammatory, and antibacterial activities. It inhibits MAO-A, MAO-B, and COMT with IC50 of 50.1, 184.6, and 26.7 μM respectively.

Serotonin hydrochloride (Serotonin HCl) is an endogenous 5-HT receptor agonist, a monoamine neurotransmitter in the CNS, and a catechol O-methyltransferase (COMT) inhibitor(Ki=44 μM).

CBHcy is a dual-substrate analogue, a specific BHMT inhibitor that causes betaine-homocysteine S-methyltransferase (BHMT) to adopt the same conformation as the ternary complex, potentially inducing the development of cysteinemia.

SU0268 is a potent and specific 8-Oxoguanine DNA glycosylase 1 (OGG1) inhibitor that regulates inflammatory responses during Pseudomonas aeruginosa infection.

Opicapone (BIA 9-1067) reduces the ATP content of the cells (IC50: 98 μM). Opicapone is an effective third-generation catechol-O-methyltransferase inhibitor for the research of Parkinson's disease and motor fluctuations.