SKLB-03220 [CAS 2852050-29-2]

SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer[1].

[2852050-29-2]

C33H40N4O4

556.7

O=C(NC1=CC=C(C)C(C2=CC(N(C3CCOCC3)CC)=C(C)C(C(NCC4=C(C)C=C(C)NC4=O)=O)=C2)=C1)C=C

Apoptosis; Histone Methyltransferase

EZH2

Room temperature