2. Epigenetics
  3. Histone Methyltransferase
  4. 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).

For research use only. We do not sell to patients.

MS8511 Chemical Structure

MS8511 Chemical Structure

CAS No. : 2866408-21-9

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Based on 1 publication(s) in Google Scholar

MS8511 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target

G9a

100 nM (IC50)

G9a

44 nM (Kd)

GLP

140 nM (IC50)

GLP

46 nM (Kd)

In Vitro

MS8511 (Compound 8, 0-100 μΜ, 10 min) selectively inhibits G9a and GLP against other PKMTs and PRMTs, with IC50 values of 100 nM (G9a) and 140 nM (GLP)[1].
MS8511 (50 min) prefers covalent modification for G9a over GLP, with Kd values of 44 nM (G9a) and 46 nM (GLP)[1].
MS8511 (0-5 μM, 24-72 h) effectively reduces the H3K9me2 mark in MDA-MB-231 and K562 cellssup>[1].
MS8511 (0.8-25 μM, 3 days) inhibits the growth of MDA-MB-231 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS8511 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231, K562 cells.
Concentration: 0.2, 1, 5 μM.
Incubation Time: 24, 48, 72 h.
Result: Reduced the H3K9me2 mark in a concentration- and time-dependent manner.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.8, 1.6, 3.1 6.3, 12.5, 25 μM.
Incubation Time: 3 days
Result: Inhibited the growth of MDA-MB-231 cells.
Molecular Weight

495.66

Formula

C28H41N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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MS8511 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS85112866408-21-9MS 8511MS-8511Histone MethyltransferaseCancersPKMTs inhibitorcovalent InhibitorsH3K9me2antiproliferationMDA-MB-231 cells.Inhibitorinhibitorinhibit

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