For research use only. Not for therapeutic Use.
MS1943(Cat No.:I016895)is a selective degrader of EZH2, an enzyme involved in epigenetic regulation. It is orally bioavailable and has demonstrated the ability to effectively reduce the levels of EZH2 in cells. MS1943 exhibits an IC50 value of 120 nM for inhibiting the methyltransferase activity of EZH2, which is responsible for its role in gene silencing. By targeting and degrading EZH2, MS1943 may have potential therapeutic applications in conditions where dysregulated EZH2 activity is implicated, such as certain cancers and other diseases involving epigenetic dysregulation.
Catalog Number | I016895 |
CAS Number | 2225938-17-8 |
Molecular Formula | C₄₂H₅₄N₈O₃ |
Purity | ≥95% |
IUPAC Name | 6-[6-[4-[2-[[2-(1-adamantyl)acetyl]amino]ethyl]piperazin-1-yl]pyridin-3-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-propan-2-ylindazole-4-carboxamide |
InChI | InChI=1S/C42H54N8O3/c1-26(2)50-37-18-33(17-34(36(37)25-46-50)40(52)45-24-35-27(3)13-28(4)47-41(35)53)32-5-6-38(44-23-32)49-11-9-48(10-12-49)8-7-43-39(51)22-42-19-29-14-30(20-42)16-31(15-29)21-42/h5-6,13,17-18,23,25-26,29-31H,7-12,14-16,19-22,24H2,1-4H3,(H,43,51)(H,45,52)(H,47,53) |
InChIKey | WQIQJFXBAJJKNT-UHFFFAOYSA-N |
SMILES | CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)CCNC(=O)CC67CC8CC(C6)CC(C8)C7)C(C)C)C |
Reference | [1]. Ma A, et al. Discovery of a first-in-class EZH2 selective degrader.Nat Chem Biol. 2020 Feb;16(2):214-222. |