2. PROTAC Epigenetics Apoptosis
  3. PROTACs Histone Methyltransferase Apoptosis
  4. 2225938-17-8

2225938-17-8

MS1943 Chemical Structure

2225938-17-8

Chemical Structure

  • MS1943
  • CAS No: 2225938-17-8
    Formula: C42H54N8O3
    Molecular Weight: 718.93
  • IUPAC Name: 6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide
  • InChIKey: WQIQJFXBAJJKNT-SIAAHZTCSA-N
  • SMILES: CC(C)N(N=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C4=CC=C(N=C4)N(CC5)CCN5CCNC(CC67C[C@H]8C[C@H](C[C@H](C8)C7)C6)=O)=C2

Biological Activity: MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578))[1].

Cat. No. Product Name Purity Description
HY-133129 MS1943 98.92% MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)).

References

[1]. Ma A, et al. Discovery of a first-in-class EZH2 selective degrader[J]. Nature chemical biology, 2020, 16(2): 214-222. [Content Brief]

Keywords:

MS1943