For research use only. Not for therapeutic Use.
MS177（Cat No.:I042627）is a potent and selective degrader of Enhancer of Zeste Homolog 2 (EZH2), designed as a Proteolysis Targeting Chimera (PROTAC). It comprises a cereblon (CRBN) ligand linked to the enzymatic EZH2 inhibitor C24, which has an IC₅₀ of 12 nM. MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes, leading to inhibition of leukemia cell growth, induction of apoptosis, and cell cycle arrest. In vitro studies show that MS177 inhibits EZH2-PRC2 enzymatic activity with an IC₅₀ of 7 nM. In vivo, MS177 suppresses acute myeloid leukemia growth without apparent toxicity in patient-derived xenograft models.
| CAS Number | 2225938-86-1 |
| Synonyms | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[6-[4-[2-[3-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]propanoylamino]ethyl]piperazin-1-yl]pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamide |
| Molecular Formula | C48H55N11O8 |
| Purity | ≥95% |
| IUPAC Name | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[6-[4-[2-[3-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]propanoylamino]ethyl]piperazin-1-yl]pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamide |
| InChI | InChI=1S/C48H55N11O8/c1-28(2)59-39-24-32(23-34(36(39)27-53-59)44(62)52-26-35-29(3)22-30(4)54-45(35)63)31-8-10-40(51-25-31)57-18-16-56(17-19-57)15-13-50-41(60)12-20-67-21-14-49-37-7-5-6-33-43(37)48(66)58(47(33)65)38-9-11-42(61)55-46(38)64/h5-8,10,22-25,27-28,38,49H,9,11-21,26H2,1-4H3,(H,50,60)(H,52,62)(H,54,63)(H,55,61,64) |
| InChIKey | LRMNSTSNSCJHGZ-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)CCOCCNC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O)C(C)C)C |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
