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MS1943 #23943

    Product Information

    Product Usage Information

    MS1943 is supplied as a lyophilized powder. For a 5 mM stock, reconstitute 5 mg of powder in 1.39 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

    Storage

    Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 718.9 g/mol
    Purity 98%
    Molecular Formula C42H54N8O3
    CAS 2225938-17-8
    Solubility Soluble in DMSO at 10 mg/mL.

    Background

    The polycomb group (PcG) proteins are involved in maintaining the silenced state of several developmentally regulated genes and contribute to the maintenance of cell identity, cell cycle regulation, and oncogenesis (1,2). Enhancer of zeste homolog 2 (Ezh2), a member of this large protein family, contains four conserved regions, including domain I, domain II, and a cysteine-rich amino acid stretch that precedes the carboxy-terminal SET domain (3). The SET domain has been linked with histone methyltransferase (HMTase) activity. Moreover, mammalian Ezh2 is a member of a histone deacetylase complex that functions in gene silencing, acting at the level of chromatin structure (4). Ezh2 complexes methylate histone H3 at Lys9 and 27 in vitro, which is thought to be involved in targeting transcriptional regulators to specific loci (5). Ezh2 is deregulated in various tumor types, and its role, both as a primary effector and as a mediator of tumorigenesis, has become a subject of increased interest (6).

    MS1943 is an Ezh2 degrader that lowers levels of Ezh2 protein in cells (7). Ezh2 degradation has proven to be effective beyond traditional methyltransferase inhibitors in certain cancers that grow independent of Ezh2 catalytic activity (7,8).
    For Research Use Only. Not for Use in Diagnostic Procedures.
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