CeMMEC1 HCl

Catalog No.S8328 Batch:S832801

Technical Data

Formula	C₁₉H₁₇ClN₂O₄
Molecular Weight	372.8	CAS No.	2095432-53-2
Solubility (25°C)*	In vitro	DMSO	23 mg/mL (61.69 mM)
		Ethanol	1 mg/mL (2.68 mM)
		Water	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

CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM).

Targets

TAF1 ^[1]
(Cell-based assay)

1.8 μM(Kd)

In vitro

CeMMEC1 only bound BRD4 very weakly but it shows high affinity for the bromodomains of CREBBP, EP300, BRD9 and the second bromodomain of TAF1^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines REDS3 cells Concentrations 10 μM Incubation Time 24 h Method REDS3 cells were treated with 10 μM of every compound, and live-cell imaging pictures were taken to assess their ability to induce RFP expression 24 h later. From this primary screening 1,286 small molecules were selected as hits and rescreened in the follow-up part, in which REDS3 and WT KBM7 cells were treated in three-point dose response in order to exclude autofluorescent or toxic compounds. 80 small molecules were selected as hits and used to treat WT KBM7 cells and REDS3 cells in eight-point dose (twofold dilution, starting from 100 μM) response and three-point time course (24 h, 48 h and 72 h) to carefully select the best true hits (time- and dose-dependent RFP expression/no autofluorescence). UPLC-MS analysis was done to confirm purity and the correct mass of the small molecules selected; finally, 22 small molecules fulfilled the criteria as screening hits.

Cell Assay:^{^[1]}

Cell lines
REDS3 cells
Concentrations
10 μM
Incubation Time
24 h
Method
REDS3 cells were treated with 10 μM of every compound, and live-cell imaging pictures were taken to assess their ability to induce RFP expression 24 h later. From this primary screening 1,286 small molecules were selected as hits and rescreened in the follow-up part, in which REDS3 and WT KBM7 cells were treated in three-point dose response in order to exclude autofluorescent or toxic compounds. 80 small molecules were selected as hits and used to treat WT KBM7 cells and REDS3 cells in eight-point dose (twofold dilution, starting from 100 μM) response and three-point time course (24 h, 48 h and 72 h) to carefully select the best true hits (time- and dose-dependent RFP expression/no autofluorescence). UPLC-MS analysis was done to confirm purity and the correct mass of the small molecules selected; finally, 22 small molecules fulfilled the criteria as screening hits.

References

[1] Sdelci S, et al. Nat Chem Biol. 2016, 12(7):504-10.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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