SETD

All (4) SETD Inhibitors (4)

Catalog No.	Information	Product Use Citations
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.	J Biol Chem, 2020, 10.1074/jbc.RA119.010951 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183 Cancer Res, 2018, 78(20):5731-5740
S7294	PFI-2 HCl PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with K_{i (app)} and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.	Brain Behav Immun, 2019, 82:382-395 Cancer Res, 2018, 78(20):5731-5740 Cell Death Dis, 2018,
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.	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

Catalog No.	Information	Product Use Citations
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.	J Biol Chem, 2020, 10.1074/jbc.RA119.010951 Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183 Cancer Res, 2018, 78(20):5731-5740
S7294	PFI-2 HCl PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with K_{i (app)} and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets.	Brain Behav Immun, 2019, 82:382-395 Cancer Res, 2018, 78(20):5731-5740 Cell Death Dis, 2018,
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.	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