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MS8511

Products Details

Product Description

– MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS)[1].

Web ID

– HY-150510

Shipping

– Room temperature

Applications

– Cancer-programmed cell death

Molecular Formula

– C28H41N5O3

References

– [1]Kwang-Su Park, et al. Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J Med Chem. 2022 Jun 28.

CAS Number

– 2866408-21-9

Molecular Weight

– 495.66

SMILES

– COC1=CC(C(C=C1OCCCN2CCCC2)=NC(NC(C=C)=O)=C3)=C3NC4CCN(CC4)C(C)C

Clinical Information

– No Development Reported

Research Area

– Cancer; Neurological Disease

Solubility

– 10 mM in DMSO

Target

– Histone Methyltransferase

Isoform

– EHMT1/GLP/KMT1D;EHMT2/G9a/KMT1C

Pathway

– Epigenetics

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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