MS8511
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].
Product Specifications
CAS Number
[2866408-21-9]
UNSPSC
12352005
Target
Histone Methyltransferase
Type
Reference compound
Related Pathways
Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/ms8511.html
Purity
99.82
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
COC1=CC(C(C=C1OCCCN2CCCC2)=NC(NC(C=C)=O)=C3)=C3NC4CCN(CC4)C(C)C
Molecular Formula
C28H41N5O3
Molecular Weight
495.66
References & Citations
[1]Kwang-Su Park, et al. Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J Med Chem. 2022 Jun 28.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C
Available Sizes
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