setd2

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

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.

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].