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CeMMEC1 Sale

目录号 : GC19098

A selective TAF1 bromodomain 2 inhibitor

CeMMEC1 Chemical Structure

Cas No.:440662-09-9

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5mg
¥540.00
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10mg
¥900.00
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25mg
¥1,980.00
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50mg
¥3,510.00
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100mg
¥6,210.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Kinase experiment:

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].

Cell experiment:

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].

References:

[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.

产品描述

CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 uM for TAF1, and a Kd of 1.8 uM for TAF1 (2).

CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 uM for TAF1, and a Kd of 1.8 uM for TAF1 (2) and slso shows high affinity for the bromodomains of CREBBP, EP300, BRD9. CeMMEC1 (1, 10, 20 uM) 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].

References:
[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.

Chemical Properties

Cas No. 440662-09-9 SDF
Canonical SMILES O=C(C(C1=C2C=CC=C1)=CN(C)C2=O)NC3=CC=C(OCCO4)C4=C3
分子式 C19H16N2O4 分子量 336.34
溶解度 DMSO : 100 mg/mL (297.32 mM) 储存条件 Store at -20°C
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1 mM 2.9732 mL 14.8659 mL 29.7318 mL
5 mM 0.5946 mL 2.9732 mL 5.9464 mL
10 mM 0.2973 mL 1.4866 mL 2.9732 mL
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