Transferase

Transferase製品

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  • Transferase阻害剤 (38)
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S2799 Daporinad (FK866) Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Cell Discov, 2024, 10(1):39
Theranostics, 2024, 14(7):2794-2815
Theranostics, 2024, 14(15):5999-6015
S8244 Etomoxir sodium salt Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.
Bioact Mater, 2024, 35:549-563
Cell Chem Biol, 2024, 31(10):1772-1786.e5
Oncogene, 2024, 43(6):406-419
S1453 Tipifarnib 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.
Cell Rep, 2023, 42(9):113098
iScience, 2023, 26(5):106695
Int J Mol Sci, 2023, 24(14)11546
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.
J Cell Biol, 2024, 223(1)e202303007
J Cell Biol, 2024, 223(1)e202303007
EMBO Rep, 2024, 25(10):4311-4336
S7465 FTI 277 HCl FTI 277 HCl is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.
Cancer Res, 2023, 83(13):2248-2261
PLoS Biol, 2021, 19(4):e3001134
Cell Struct Funct, 2021, 46(1):1-9
S7466 GGTI 298 TFA salt GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.
bioRxiv, 2024, 10.1101/2024.01.16.575899
Nat Commun, 2023, 14(1):3251
Cell Struct Funct, 2021, 46(1):1-9
S4989 AOA (Aminooxyacetic acid) hemihydrochloride AOA (Aminooxyacetic acid) hemihydrochloride is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. AOA hemihydrochloride is also a CBS (cystathionine β-synthase) inhibitor.
Research Square, 2024, 10.21203/rs.3.rs-3849836/v1
Cell Rep Med, 2023, 4(5):101026
EMBO Mol Med, 2023, e15674.
S8608 ADOX (Adenosine Dialdehyde) ADOX (Adenosine Dialdehyde) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.
Nat Commun, 2024, 15(1):8971
EMBO J, 2023, e114558.
PLoS Biol, 2022, 20(2):e3001535
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. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
Mol Metab, 2022, 65:101597
S9870 STM2457 STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases.
Nat Commun, 2024, 15(1):8539
Cell Rep, 2024, 43(2):113796
Cell Mol Biol Lett, 2024, 29(1):106
S7894 Tunicamycin Tunicamycin, an antibiotic, can potently inhibit the N-linked glycosylation (NLG) by competitively inhibiting UDP-GlcNAc-dolichol-phosphate N-acetylglucosamine-1 phosphate transferase (DPAGT1) activity and can target several types of tumors by reducing angiogenesis, inhibiting colony formation, and enhancing TRAIL-induced apoptosis.
Cell Discov, 2023, 9(1):92
Cell Discov, 2023, 9(1):92
Adv Sci (Weinh), 2023, 10(25):e2300414
S4589 Amodiaquine dihydrochloride dihydrate Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent.
Cell Death Differ, 2023, 10.1038/s41418-023-01167-4
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
J Med Chem, 2020, 31
S8910 OSMI-4 OSMI-4 is an inhibitor of O-linked N-acetylglucosamine transferase (O-GlcNAc transferase, OGT) with EC50 of 3 μM in cells.
Elife, 2023, 12e85595
Sci Adv, 2023, 9(33):eadg7112
Sci Adv, 2023, 9(33):eadg7112
S2674 A922500 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.
Nature, 2023, 621(7977):171-178
Nature, 2023, 621(7977):171-178
Cell Rep, 2022, 41(11):111827
S4021 Tolcapone Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
FASEB J, 2022, 36(7):e22399
Viruses, 2021, 13(8)1533
Front Bioinform, 2021, 1:710591
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; Also inhibits N-acetyltransferase.
Cancers -Basel, 2022, 14-174200
J Surg Res, 2021, 263:236-244
Exp Ther Med, 2015, 10(3):1066-1070
E0081 FIDAS-3 FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for methionine sadenosyltransferase 2A (MAT2A) binding . FIDAS-3 has anticancer activities by inhibiting the expression of oncogenes. FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for MAT2A.
Cell Death Dis, 2023, 14(8):525
Cell Death Dis, 2023, 14(8):525
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.
Aging Dis, 2023, 14(5):1927-1944
Aging Dis, 2023, 14(5):1927-1944
S7192 PF-04620110 PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
J Pharm Biomed Anal, 2019, 170:176-186
J Cell Biol, 2018, 217(3):975-995
E0120 2-BP (2-Bromohexadecanoic acid) 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.
Cell Mol Biol Lett, 2024, 29(1):112
J Virol, 2024, 98(4):e0164923
Cancer Res, 2023, 83(12):2034-2051
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).
Cell Death Dis, 2024, 15(4):244
Biomed Res Int, 2020, 2020:1921609
S2994 DL-Homocysteine

DL-Homocysteine is a weak neurotoxin that affects the production of kynurenic acid (KYNA) in the brain. DL-Homocysteine inhibits the activity of both KYNA biosynthetic enzymes, kynurenine aminotransferases (KATs) I and II.

E1029 Miglustat Miglustat (Zavesca, N‐butyldeoxynojirimycin, OGT 918) is an orally administered ceramide glucosyltransferase inhibitor which prevents the lysosomal accumulation of glucocerebroside.
S9231 Schisanhenol Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7.
Exploratory Research and Hypothesis in Medicine, 2023, 10.14218/ERHM.2023.00054
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.
S9698 Ezatiostat Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces 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.
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.
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)
S0359 T863 (DGAT-3) T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells.
E4639New 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. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 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.
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.
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
S5166 Benzoyleneurea Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors.
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. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).
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.
S6392New SHIN1(RZ-2994) SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with IC50 values of 5 and 13 nM, respectively, in in vitro assay. SHIN1 hinders cell growth by gradually reducing purine levels.
S2799 Daporinad (FK866) Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Cell Discov, 2024, 10(1):39
Theranostics, 2024, 14(7):2794-2815
Theranostics, 2024, 14(15):5999-6015
S8244 Etomoxir sodium salt Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.
Bioact Mater, 2024, 35:549-563
Cell Chem Biol, 2024, 31(10):1772-1786.e5
Oncogene, 2024, 43(6):406-419
S1453 Tipifarnib 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.
Cell Rep, 2023, 42(9):113098
iScience, 2023, 26(5):106695
Int J Mol Sci, 2023, 24(14)11546
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.
J Cell Biol, 2024, 223(1)e202303007
J Cell Biol, 2024, 223(1)e202303007
EMBO Rep, 2024, 25(10):4311-4336
S7465 FTI 277 HCl FTI 277 HCl is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.
Cancer Res, 2023, 83(13):2248-2261
PLoS Biol, 2021, 19(4):e3001134
Cell Struct Funct, 2021, 46(1):1-9
S7466 GGTI 298 TFA salt GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.
bioRxiv, 2024, 10.1101/2024.01.16.575899
Nat Commun, 2023, 14(1):3251
Cell Struct Funct, 2021, 46(1):1-9
S4989 AOA (Aminooxyacetic acid) hemihydrochloride AOA (Aminooxyacetic acid) hemihydrochloride is an inhibitor of aminobutyrate aminotransferase involved in amino acid and polyamine metabolism. AOA hemihydrochloride is also a CBS (cystathionine β-synthase) inhibitor.
Research Square, 2024, 10.21203/rs.3.rs-3849836/v1
Cell Rep Med, 2023, 4(5):101026
EMBO Mol Med, 2023, e15674.
S8608 ADOX (Adenosine Dialdehyde) ADOX (Adenosine Dialdehyde) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.
Nat Commun, 2024, 15(1):8971
EMBO J, 2023, e114558.
PLoS Biol, 2022, 20(2):e3001535
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. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
Mol Metab, 2022, 65:101597
S9870 STM2457 STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases.
Nat Commun, 2024, 15(1):8539
Cell Rep, 2024, 43(2):113796
Cell Mol Biol Lett, 2024, 29(1):106
S7894 Tunicamycin Tunicamycin, an antibiotic, can potently inhibit the N-linked glycosylation (NLG) by competitively inhibiting UDP-GlcNAc-dolichol-phosphate N-acetylglucosamine-1 phosphate transferase (DPAGT1) activity and can target several types of tumors by reducing angiogenesis, inhibiting colony formation, and enhancing TRAIL-induced apoptosis.
Cell Discov, 2023, 9(1):92
Cell Discov, 2023, 9(1):92
Adv Sci (Weinh), 2023, 10(25):e2300414
S4589 Amodiaquine dihydrochloride dihydrate Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent.
Cell Death Differ, 2023, 10.1038/s41418-023-01167-4
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
J Med Chem, 2020, 31
S8910 OSMI-4 OSMI-4 is an inhibitor of O-linked N-acetylglucosamine transferase (O-GlcNAc transferase, OGT) with EC50 of 3 μM in cells.
Elife, 2023, 12e85595
Sci Adv, 2023, 9(33):eadg7112
Sci Adv, 2023, 9(33):eadg7112
S2674 A922500 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.
Nature, 2023, 621(7977):171-178
Nature, 2023, 621(7977):171-178
Cell Rep, 2022, 41(11):111827
S4021 Tolcapone Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
FASEB J, 2022, 36(7):e22399
Viruses, 2021, 13(8)1533
Front Bioinform, 2021, 1:710591
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; Also inhibits N-acetyltransferase.
Cancers -Basel, 2022, 14-174200
J Surg Res, 2021, 263:236-244
Exp Ther Med, 2015, 10(3):1066-1070
E0081 FIDAS-3 FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for methionine sadenosyltransferase 2A (MAT2A) binding . FIDAS-3 has anticancer activities by inhibiting the expression of oncogenes. FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for MAT2A.
Cell Death Dis, 2023, 14(8):525
Cell Death Dis, 2023, 14(8):525
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.
Aging Dis, 2023, 14(5):1927-1944
Aging Dis, 2023, 14(5):1927-1944
S7192 PF-04620110 PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
J Pharm Biomed Anal, 2019, 170:176-186
J Cell Biol, 2018, 217(3):975-995
E0120 2-BP (2-Bromohexadecanoic acid) 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.
Cell Mol Biol Lett, 2024, 29(1):112
J Virol, 2024, 98(4):e0164923
Cancer Res, 2023, 83(12):2034-2051
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).
Cell Death Dis, 2024, 15(4):244
Biomed Res Int, 2020, 2020:1921609
S2994 DL-Homocysteine

DL-Homocysteine is a weak neurotoxin that affects the production of kynurenic acid (KYNA) in the brain. DL-Homocysteine inhibits the activity of both KYNA biosynthetic enzymes, kynurenine aminotransferases (KATs) I and II.

E1029 Miglustat Miglustat (Zavesca, N‐butyldeoxynojirimycin, OGT 918) is an orally administered ceramide glucosyltransferase inhibitor which prevents the lysosomal accumulation of glucocerebroside.
S9231 Schisanhenol Schisanhenol (Gomisin K3) is a compound derived from the fruit of a traditional Chinese herb Schisandra rubriflora, exhibiting strong inhibition toward UGT2B7.
Exploratory Research and Hypothesis in Medicine, 2023, 10.14218/ERHM.2023.00054
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.
S9698 Ezatiostat Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces 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.
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.
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)
S0359 T863 (DGAT-3) T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells.
E4639New 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. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 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.
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.
Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0221
S5166 Benzoyleneurea Benzoyleneurea (2,4-Dihydroxyquinazoline, Quinazolinedione, Quinazoline-2,4-diol) scaffold is used in the synthesis of novel protein geranylgeranyltransferase-I inhibitors.
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. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).
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.
S6392New SHIN1(RZ-2994) SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with IC50 values of 5 and 13 nM, respectively, in in vitro assay. SHIN1 hinders cell growth by gradually reducing purine levels.
E4639New 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. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 also demonstrates anticancer activity.
S6392New SHIN1(RZ-2994) SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with IC50 values of 5 and 13 nM, respectively, in in vitro assay. SHIN1 hinders cell growth by gradually reducing purine levels.

Transferase阻害剤の選択性比較

Transferaseシグナル伝達経路

Transferaseシグナル伝達経路
Tags: Transferase activity | Transferase inhibition | Transferase activity | protein transferase | farnesyltransferase | DNA methyltransferase cancer | DNA methyltransferase activity | DNA methyltransferase assay | DNA methyltransferase mechanism | farnesyl transferase assay | Transferase inhibitor review