CeMMEC1 MedChemExpress (MCE)

Product Name	CeMMEC1 HCl
Synonyms	CeMMEC1;cemmecl;CeMMEC1 HCl;440662-09-9;CeMMEC1(free base);4-Isoquinolinecarboxamide, N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1,2-dihydro-2-methyl-1-oxo-
CAS	440662-09-9
EINECS
Chemical Formula	C19H16N2O4
Molecular Weight	336.34
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	CeMMEC1 CeMMEC1 MedChemExpress (MCE) HY-111445 440662-09-9 99.65% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions CeMMEC1 CeMMEC1 MedChemExpress (MCE) HY-111445 440662-09-9 99.65% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2). CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2) and slso shows high affinity for the bromodomains of CREBBP, EP300, BRD9. CeMMEC1 (1, 10, 20 μM) decreases the number of THP1 cells in S phase in a dose manner. CeMMEC1 also induces apoptosis. CeMMEC1 in combination with (S)-JQ1 displays potently impaired cell viability than treatment alone[1]. Cells are seeded on clear flat-bottom 96-well or 384-well plates and treated with the indicated compounds (CeMMEC1) for the specified conditions. Live-cell imaging pictures are taken with the Operetta High Content Screening System, 20× objective and nonconfocal mode[1]. TAF1 binding assays are conducted using the EPIgeneous Binding Domain kit B. Binding is determined by the displacement of an acetylated biotin peptide from a GST-tagged TAF1 protein using HTRF with a Eu3+-conjugated GST antibody donor and streptavidin-conjugated acceptor. Compounds (CeMMEC1) are dispensed into assay plates, ProxiPlate-384 Plus using an Echo 525 Liquid Handler. Binding assays are conducted in a final volume of 20 μL with 5 nM TAF1-GST, 50 nM peptide (SGRGK (ac)GGK (ac)GLGK (ac)GGAK (ac)RHRK (biotin)-acid), 6.25 nM Streptavidin-XL665, 1:200 Anti-GST-Eu3+ cryptate and 0.1% DMSO. Assay reagents are dispensed into plates using a Multidrop combi and incubated at room temperature for 3 h. Fluorescence is measured using a PHERAstar microplate reader using the HTRF module with dual emission protocol (A = excitation of 320 nm, emmission of 665 nm, and B = excitation of 320 nm, emission of 620 nm). Raw data are processed to give an HTRF ratio (channel A/B × 10,000), which is used to generate IC50 curves[1]. Kd: 1.8 μM (TAF1 (2))[1] IC50: 0.9 μM (TAF1)[1] In Vitro CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2) and slso shows high affinity for the bromodomains of CREBBP, EP300, BRD9. CeMMEC1 (1, 10, 20 μM) decreases the number of THP1 cells in S phase in a dose manner. CeMMEC1 also induces apoptosis. CeMMEC1 in combination with (S)-JQ1 displays potently impaired cell viability than treatment alone[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CeMMEC1 Related Antibodies \| \| \| \| \| \| \| \| \| \| [1]. Sdelci S, et al. Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nat Chem Biol. 2016 Jul 12(7):504-10. [Content Brief]
Last Update	2025-04-01 14:45:47

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