MAK683

Catalog No.S8983 Batch:S898301

Technical Data

Formula	C₂₀H₁₇FN₆O
Molecular Weight	376.39	CAS No.	1951408-58-4
Solubility (25°C)*	In vitro	DMSO	12.5 mg/mL (33.21 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:^{^[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.

Cell Assay:^{^[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.

References

Selleck's MAK683 has been cited by 3 publications

Combating castration-resistant prostate cancer by co-targeting the epigenetic regulators EZH2 and HDAC [ PLoS Biol, 2023, 21(4):e3002038]	PubMed: 37104245
Induction of senescence-associated secretory phenotype underlies the therapeutic efficacy of PRC2 inhibition in cancer [ Cell Death Dis, 2022, 13(2):155]	PubMed: 35169119
ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors [ JCI Insight, 2022, e155899]	PubMed: 35852858

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SHIPPING AND STORAGE
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