MS177

MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50) : 12 nM) . MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest[1].

Product Specifications

CAS Number

[2225938-86-1]

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ms177.html

Purity

99.55

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(C2=CC=C(N3CCN(CCNC(CCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)CC3)N=C2)=CC7=C1C=NN7C(C)C)NCC8=C(C)C=C(C)NC8=O

Molecular Formula

C48H55N11O8

Molecular Weight

914.02

References & Citations

[1]Wang J, et al. EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis. Nat Cell Biol. 2022 Mar;24 (3) :384-399.