Transferase Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| E0120 | 2-Bromohexadecanoic acid (2-BP) | 2-BP (2-Bromohexadecanoic acid) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor, which inhibits multiple palmitoyl-acyl Transferase (PAT) activity towards MyrGCK(NBD) and FarnCNRas(NBD) with identical IC50s of approx. 4 µM. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins. |
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| S2674 | A-922500 (DGAT-1 Inhibitor 4a) | A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
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| S9835 | OSMI-1 | OSMI-1 is a cell-permeable O-GlcNAc Transferase (OGT) inhibitor with IC50 of 2.7 μM for full length human OGT (ncOGT). |
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| S7192 | PF-04620110 | PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
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| S9231 | Schisanhenol | Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7. |
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| S3945 | L-Cycloserine | L-Cycloserine (Levcycloserine, Levcicloserina, Levcycloserinum, (-)-Cycloserine, (S)-Cycloserine) is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity. |
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| E0081 | FIDAS-3 | FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for methionine sadenosyltransferase 2A (MAT2A) binding. This compound has anticancer activities by inhibiting the expression of oncogenes. It is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for MAT2A. |
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| E1017 | ERG240 | ERG240, a selective inhibitor of branched-chain aminotransferase 1 (BCAT1) with an IC50 of 0.1-1nM, leads to decreased oxygen consumption and glycolysis through the down regulation of IRG1 expression, which leads to decrease itaconate production in human macrophages. |
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| S9954 | SGN-2FF |
SGN-2FF (2-fluorofucose) is an orally bioavailable small-molecule inhibitor of fucosyltransferase that demonstrated encouraging preclinical antitumor activity in mouse models. |
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| S6392 | SHIN1(RZ-2994) | SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with respective IC50 values of 5 and 13 nM in in vitro assays. It hinders cell growth by gradually reducing purine levels. |
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| S2994 | DL-Homocysteine |
DL-Homocysteine is a weak neurotoxin that affects the production of kynurenic acid (KYNA) in the brain. This compound inhibits the activity of both KYNA biosynthetic enzymes, kynurenine aminotransferases (KATs) I and II. |
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| S0970 | Curzerene | Curzerene, a sesquiterpene isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity, inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression and induces cell apoptosis. | ||
| S5336 | Hecogenin | Hecogenin (Hocogenin), a steroid saponin isolated from Agave sisalana, is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1.5 μM. | ||
| E0405 | L002 (NSC764414) | L002 (NSC764414) is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. | ||
| S5449 | 3-Methoxybenzamide | 3-Methoxybenzamide (3-MBA) is a competitive inhibitor of poly(ADP-ribose) synthetase with Ki values of less than 2 μM and also inhibits ADP-ribosyltransferase (ADPRT) | ||
| E4639 | FIDAS-5 | FIDAS-5 is a potent and orally active inhibitor of methionine S-adenosyltransferase 2A (MAT2A) with an IC50 value of 2.1 μM, respectively. This compound effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. It also demonstrates anticancer activity. | ||
| S4189 | Cyclandelate | Cyclandelate (BS 572,3,5,5-Trimethylcyclohexyl mandelate) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol Acyltransferase (ACAT) with IC50 of 80 μM. | ||
| S5166 | Benzoyleneurea | Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors. This compound possesses anti-Bacterial activity. | ||
| E6008 | Miglustat hydrochloride | Miglustat hydrochloride (N-Butyldeoxynojirimycin hydrochloride) is an effective, reversible, and non-toxic iminosugar and an inhibitor of ceramide-specific glucosyl transferase and β-glucosidase 2, with an IC50 of 32 μM and 81 μM, respectively. It is used in the treatment and research of dyslipidosis-related disorders, including GM1 gangliosidosis, Gaucher type I, Tay-Sachs disease, and Niemann-Pick type C disease (NPCD). | ||
| S4280 | Meclofenoxate (Centrophenoxine) HCl | Meclofenoxate (Centrophenoxine) HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase. | ||
| S1453 | Tipifarnib (IND 58359) | Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3. |
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| S2797 | Lonafarnib (SCH66336) | Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
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| S3021 | Rimonabant (SR141716) | Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane, and it is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 that inhibits mycobacterial MmpL3. |
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| S9849 | EIPA (L593754) | EIPA (L593754; MH 12-43) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis. |
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| S4589 | Amodiaquine dihydrochloride dihydrate | Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent. |
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| S4743 | Wogonin | Wogonin (Vogonin), a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; This compound also inhibits N-acetyltransferase. |
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| S4021 | Tolcapone | Tolcapone (Ro 40-7592) is a selective, potent and reversible catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM. |
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| S0359 | T863 (DGAT-3) | T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) that acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells. |
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| S7467 | LB42708 | LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively. |
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| E1029 | Miglustat (N-Butyldeoxynojirimycin) |
Miglustat (Zavesca, N-butyldeoxynojirimycin, OGT 918) is an orally administered ceramide glucosyltransferase inhibitor which prevents the lysosomal accumulation of glucocerebroside. |
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| E1944 | Rentosertib (INS018-055, ISM001-055) | INS018-055 (ISM001-055, TNIK&MAP4K4-IN-2, compound 112) is an inhibitor of TNIK and MAP4K4. It exhibits IC50 values of 12-120 nM on TNIK. | ||
| S6886 | 1-Aminobenzotriazole | 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. This compound is also a substrate and inhibitor of N-acetyltransferase (NAT). |
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