SMYD3 Inhibitor

EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC₅₀ value of 3 nM. EPZ031686 can be used for cancer research.

BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.

BAY-6035, a chemical probe, is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC₅₀ of 88 nM.

EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (K_D=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours.

GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a K_i of 14 nM and an IC₅₀ of 130 nM.

SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC₅₀ of 11.7 nM.

SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC₅₀ values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer.