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.

Serotonin (5-hydroxytryptamine) is a natural product from animals

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.

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.

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.

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

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

Nizubaglustat (AZ3102) is an orally available, selective and brain-permeable dual inhibitor of ceramide glucosyltransferase and non-lysosomal glucosylceramide amidase (NLGase) for the study of neurological diseases.

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).

CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity. It inhibits farnesylation of recombinant human H-Ras (IC50=0.57 ng mL) and K-Ras (IC50=46 ng mL)[1]. In 3T3 H-ras (61L)-transfected cell lines, CP-609754 exhibits a slow on off rate, inhibiting mutant H-Ras farnesylation with an IC50 of 1.72 ng mL[1]. The compound is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI, selectively inhibiting farnesylation of both H- and K-Ras proteins in 3T3 transfectants[1]. In vivo, CP-609754 shows antitumor activity against 3T3 H-ras (61L) tumors, with tumor regression achieved at 100 mg kg twice daily and an ED50 for tumor growth inhibition at 28 mg kg[1]. Continuous i.p. infusion of CP-609754 inhibits tumor growth by over 50% and reduces tumor farnesyltransferase activity by over 30% when plasma concentration is maintained above 118 ng mL[1]. [1]. Stacy L Moulder, et al. A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors. Clin Cancer Res. 2004 Nov 1;10(21):7127-35.

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.

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.

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.

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

P-3FAX-Neu5Ac is a sialic acid analog and a sialyltransferase inhibitor.

Entacapone is a potent and specific peripheral catechol-O-methyltransferase (COMT) inhibitor with an IC50 of 151 nM. Entacapone is also a potential obesity-related gene (FTO) inhibitor that can inhibit FTO demethylation activity and be used in the study of metabolic diseases.

GPAT-IN-1 is a glycerol 3-phosphate acyltransferase (GPAT) inhibitor, which can be used to study obesity and diabetes.

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.

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8 1.2 2.0 nM toward H N K-ras).

FSG67 is a glycerol 3-phosphate acyltransferase (GPAT) and glycerol-3-phosphate acyltransferase, mitochondrial (GPAM) inhibitor that attenuates hepatic regeneration following acetaminophen overdose by altering GSK3β and Wnt β-catenin signaling.

BMS-214662 is a selective farnesyl transferase inhibitor with antitumor activity, useful in studies of pancreatic, head and neck, and lung cancers.

OU749 is a γ-glutamyl transferase (GGT) inhibitor with an intrinsic Ki of 17.6 μM.

Miglustat hydrochloride (N-Butyldeoxynojirimycin hydrochloride) is an inhibitor of glucosylceramide synthase and can be used for studies about Type I Gaucher disease.

GGsTop (Nahlsgen) is a highly selective and irreversible inhibitor of γ-glutamyltransferase (GGT) with antiaging activity.

Tipifarnib S enantiomer ((S)-(-)-R-115777) is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase inhibitor (IC50: 0.6 nM).

Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor. Ervogastat reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).

Tectol has anti-plasmodial activity, it as a moderately active growth inhibitor with an IC50 3.44±0.20μM. It exhibited significant activity against human leukemia cell lines HL60 and CEM. Tectol may cause itchy dermatitis, the dermatitis appeared on the n

GGTI298 Trifluoroacetate (GGTI 298 TFA salt) is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.

Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.

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).

FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

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

The L-778123 hydrochloride is an inhibitor of FPTase (IC50: 2 nM) and GGPTase-I (IC50: 98 nM) in enzyme inhibition determination.

Tolcapone (Ro 40-7592) is a catechol-O-methyltransferase inhibitor employed as an adjunctive therapy with levodopa and carbidopa in the treatment of Parkinson's disease.

FDW028 is a selective and potent fucosyltransferase 8 (FUT8) inhibitor with anti-tumor activity that drives B7-H3 lysosomal degradation via defucosylation and CMA pathways. FUT8 can be used to study metastatic colorectal cancer (mCRC).

ABT-046 is an orally active, selective, and highly efficient Diacylglycerol Acyltransferase 1 (DGAT-1) inhibitor that can be used in metabolic disease research.

DGAT1-IN-1 is a potent inhibitor of diacylglycerol O-acyltransferase type 1 (DGAT1) with an IC50 of less than 10 nM.

Alendronate sodium hydrate (MK 217) is a nitrogen-containing bisphosphonate, which is an effective inhibitor of bone resorption. It is utilized for the treatment and prevention of osteoporosis.

GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors.

Acivicin hydrochloride is the hydrochloride form of Acivicin (AT125, U42126).Acivicin, a natural product from Streptomyces sviceus (Streptomyces), is a glutamine analog and a potent inhibitor of γ-glutamyltransferase (GGT) and a potent inhibitor of l -Asparagine synthetase and other l-glutamine aminotransferases, and is cytotoxic by blocking nucleotide biosynthesis.

DGAT-1 inhibitor 2 is an effective DGAT-1 inhibitor and anti-obesity drug. DGAT-1 (acyl-CoA: diacylglycerol acyltransferase 1) is one of two known DGAT enzymes that catalyze the final step of triglyceride synthesis. Transgenic mice and pharmacological studies indicate that inhibiting DGAT1 is a promising strategy for treating obesity and type 2 diabetes.

JNJ-DGAT2-A, a specific inhibitor of DGAT2(IC50 = 0.14 μM), can be used in studies about the synthesis of triglycerides.

Nialamide (Nialamid) is an MAO inhibitor that is used as an antidepressive agent.

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

Rosmarinate acid(Rosemary acid) inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively

Flopropione (Phloropropiophenone), a spasmolytic or antispasmodic agent, is used as a 5-HT1A receptor antagonist.