SETD

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Catalog No. Product Name Information Product Use Citations Product Validations
S4635 Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.
Anticancer Res, 2019, 39(7):3767-3775
S7294 PFI-2 HCl PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
Pharmacol Res, 2022, 177:106122
Brain Behav Immun, 2019, 82:382-395
Cancer Res, 2018, 78(20):5731-5740
S7570 UNC0379 UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM, high selectivity over 15 other methyltransferases.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab140
J Biol Chem, 2020, 10.1074/jbc.RA119.010951
Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S7983 A-196 A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
PLoS One, 2021, 16(6):e0252504
J Immunother Cancer, 2019, 7(1):277
Nucleic Acids Res, 2019, 47(21):10977-10993
S4635 Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.
Anticancer Res, 2019, 39(7):3767-3775
S7294 PFI-2 HCl PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.
Pharmacol Res, 2022, 177:106122
Brain Behav Immun, 2019, 82:382-395
Cancer Res, 2018, 78(20):5731-5740
S7570 UNC0379 UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM, high selectivity over 15 other methyltransferases.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab140
J Biol Chem, 2020, 10.1074/jbc.RA119.010951
Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S7983 A-196 A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
PLoS One, 2021, 16(6):e0252504
J Immunother Cancer, 2019, 7(1):277
Nucleic Acids Res, 2019, 47(21):10977-10993
Tags: SETD inhibitor | SETD activator | SETD inhibition