MAK683

Catalog No.S8983 Synonyms: EED inhibitor-1

For research use only.

MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.

MAK683 Chemical Structure

CAS No. 1951408-58-4

Selleck's MAK683 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.
Targets
EED [1]
(ELISA assay)
EED [1]
(EED Alphascreen binding assay)
EED [1]
(LC-MS assay)
26 nM 59 nM 89 nM
In vitro

MAK-683 binds to EED and disrupts the PRC2 complex. Cell viability is not significantly affected and the levels of H3K27me3 are decreased. A significant increase in the percentage of mature PCs after MAK-683 treatment in association with a higher CD38 expression is also identified.[3]

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: MBCs
  • Concentrations: 2 µM
  • Incubation Time: 4 days, 3 days
  • Method:

    MBCs are differentiated using a previously described culture protocol. All cultures are performed in Iscove modified Dulbecco medium, 10% FCS and 25–35% of Resto-6 cells supernatant. 1.5 × 105/ml purified peripheral blood MBCs are activated for 4 days by 10 µg/ml of phosphorothioate CpG oligodeoxynucleotides (ODN) 2006, 50 ng/ml histidine tagged soluble CD40 ligand (CD40L) and 5 µg/ml of an anti-poly-histidine mAb in the presence of 20 U/ml IL-2, 50 ng/ml IL-10, and 10 ng/ml IL-15. The next 3 days, PBs are generated by removing ODN and CD40L and changing the cytokine cocktail. From day 7 to day 10, PBs are differentiated into early PCs by adding 50 ng/ml IL-6, 10 ng/ml IL-15, 500 U/ml IFN-α. MAK-683 (2 µM) is added at the start of each step and its effects are evaluated by analyzing cell counts and phenotype at the end of each step.

Solubility (25°C)

In vitro

DMSO 20 mg/mL
(53.13 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 376.39
Formula

C20H17FN6O

CAS No. 1951408-58-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02900651 Recruiting Drug: MAK683 Diffuse Large B-cell Lymphoma Novartis Pharmaceuticals|Novartis October 3 2016 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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