setd2

EZM0414 TFA (SETD2-IN-1 TFA) is a SETD2 inhibitor with anticancer and antiproliferative effects for the study of leukemia and immune dysfunction.

EZM0414 is a potent and selective, orally bioavailable inhibitor of SETD2 with an IC50 of 18 nM in biochemical assays and 34 nM in cellular assays, potentially useful for researching relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma [1].

MMSET-IN-1 is an inhibitor of multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) .

AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity, blocking cell proliferation, inducing apoptosis and differentiation, downregulating MLL fusion target genes, and reducing the leukemia burden in vivo[1].

AS-99 TFA is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. It blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1].

EPZ-719 is a highly selective and potent inhibitor of SETD2, a novel compound known for its ability to inhibit the enzymatic activity of SETD2 (IC50 = 0.005 μM). This compound displays a remarkable selectivity over other histone methyltransferases, making it a promising candidate for targeted therapeutic applications in the field of epigenetic research.

ssK36 is a super-substrate peptide derived from the histone methyltransferase (SET) domain protein 2 (SETD2). This peptide was specifically designed for SETD2, a unique PKMT responsible for methylating the 36th lysine residue on histone H3 (H3K36) in human cells, resulting in H3K36me3. Remarkably, ssK36 undergoes methylation by SETD2 at a rate over 100 times faster than the natural substrate H3K36. ssK36 serves as a valuable tool for investigating the catalytic mechanisms of PKMTs, particularly regarding substrate specificity and catalytic efficiency.