A PROTAC that drives EZH2 degradation
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MS1943

Item No. 35466

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-[2-[(2-tricyclo[3.3.1.13,7]dec-1-ylacetyl)amino]ethyl]-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide
CAS Number
2225938-17-8
Molecular Formula
C42H54N8O3
Formula Weight
718.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): insol
λmax
228, 284, 317 nm
SMILES
CC(C)N1N=CC2=C(C=C(C3=CC=C(N4CCN(CC4)CCNC(CC56CC7CC(C6)CC(C5)C7)=O)N=C3)C=C21)C(NCC8=C(C)C=C(C)NC8=O)=O
InChi Code
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)
InChi Key
WQIQJFXBAJJKNT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $106

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    10 mg

    $176

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    25 mg

    $352

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    Cayman Chemical
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    Product Description

    MS1943 is a proteolysis-targeting chimera (PROTAC) that contains the selective enhancer of zeste homolog 2 (EZH2) inhibitor C24 linked to an adamantyl group.1 It inhibits EZH2 (IC50 = 120 nM) and is selective for EZH2 over EZH1, as well as a panel of 45 kinases at 10 µM. MS1943 (4 µM) induces EZH2 degradation and reduces histone H3 lysine 27 trimethylation (H3K27me3), as well as induces activation of the unfolded protein response pathway in MDA-MB-468 triple-negative breast cancer (TNBC) cells. It inhibits the growth of MDA-MB-468 cells in vitro (GI50 = 2.2 µM) and reduces tumor volume in an MDA-MB-468 mouse xenograft model when administered at a dose of 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ma, A., Stratikopoulos, E., Park, K.-S., et al. Discovery of a first-in-class EZH2 selective degrader. Nat. Chem. Biol. 16(2), 214-222 (2020).