SKLB-03220
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].
Product Specifications
CAS Number
2852050-29-2
UNSPSC
12352005
Target
Apoptosis; Histone Methyltransferase
Related Pathways
Apoptosis; Epigenetics
Field of Research
Cancer
Smiles
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
Molecular Formula
C33H40N4O4
Molecular Weight
556.70
References & Citations
[1]Zhang Q, et al. Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer. J Med Chem. 2023 Feb 9;66 (3) :1725-1741.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EZH2
Frequently Asked Questions
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