High affinity inhibitor of phenylethanolamine-N-methyltransferase (PNMT) (Ki = 0.09 μM in vitro). Suppresses the release of growth hormone in an in vivo rat model.

for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities[1][2].

L-Glutamic acid γ-(p-nitroanilide) is a substrate for γ-glutamyl transpeptidase.

L-778123 HCl is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.

K-604 is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor. K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. 102.85 μ M against human ACAT1 and ACAT2, respectively) and acyl-CoA-competitive (Ki = 378 nM against oleoyl-coA) manner.

L-Glutamic acid γ-(p-nitroanilide) HCl is a substrate for GGT (gamma-glutamyltransferase), which is a transferase that catalyzes the transfer of gamma-glutamyl functional groups from molecules such as glutathione to an acceptor.

CP-609754, also known as CP-609,754, LNK 754 and OSI 754, is a selective inhibitor of arnesyltransferase with potential anticancer activity.

SHIN1 is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay.

AG-270 is a first-in-Class Oral MAT2A Inhibitor.

Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research.

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors[1].

Tipifarnib is an inhibitor of farnesyltransferase with IC50 of 0.6 nM.

FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities[1].

PF-9366 is an allosteric inhibitor of Mat2A that binds an allosteric site on Mat2A that overlaps with the binding site for the Mat2A regulator, Mat2B, targeting S-adenosylmethionine biosynthesis, with IC50 of 420 nM and Kd of 170 nM, respectively.

AG-270 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with potential antineoplastic activity.

Benzoyleneurea scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors.

EPZ015666 is a selective inhibitor of PRMT5 with Ki of 5 nM.

Perhexiline is a carnitine palmitoyltransferase 1 (CPT1) and CPT2 inhibitor that was originally developed as an anti-anginal drug.