| E1179 |
EZM0414
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EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2.
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| S7570 |
UNC0379
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UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases.
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Mol Cancer, 2025, 24(1):102
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Cell Death Dis, 2025, 16(1):226
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Res Sq, 2024, rs.3.rs-4603170
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| S7983 |
A-196
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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.
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iScience, 2023, 26(3):106158
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Cancer Res, 2022, 82(8):1534-1547
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Sci Total Environ, 2022, 838(Pt 1):155713
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| 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.
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Biochem Biophys Res Commun, 2024, 708:149808
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Life Sci Alliance, 2023, 6(5)e202201619
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Pharmacol Res, 2022, 177:106122
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| S4635 |
Cyproheptadine hydrochloride sesquihydrate
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Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.
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Anticancer Res, 2019, 39(7):3767-3775
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