Home Epigenetics Epigenetic Reader Domain inhibitor - Histone Acetyltransferase inhibitor NEO2734 For research use only.

NEO2734

Synonyms: EP31670

NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.

NEO2734 Chemical Structure

NEO2734 Chemical Structure

CAS No. 2081072-29-7

Purity & Quality Control

NEO2734 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Biological Activity

Description NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM.
Targets
p300/CBP [1]
(Cell-free assay)		 BET [1]
(Cell-free assay)
<30 nM <30 nM
In vitro
In vitro

Treatment of NMC cells with the novel dual p300/CBP and BET bromodomain–selective inhibitor, NEO2734, potently inhibits growth and induces differentiation of NMC cells in vitro; findings that correspond with potentiated transcriptional effects from combined BET and p300 bromodomain inhibition.[1]
Cell Research Cell lines NUT carcinoma patient cell lines (TC-797, 14169, 10-15, PER-403)
Concentrations 1 μM
Incubation Time 24 h
Method

NUT carcinoma patient cell lines (TC-797, 14169, 10-15, and PER-403) are plated in T-25 flasks and grown in DMEM (797) containing 10 % fetal bovine serum and 1 % penicillin/streptomycin. Cells are treated with either 500 nM OTX-015, 1 μM GNE-781, combination of 62.5 nM GNE-781 and 62.5 nM OTX-015, 1 μM NEO2734, or the equivalent volume of DMSO (0.025 %). At 24H, 2 × 106 cells are spun at 500 × g for 5 minutes at 4 ℃ and washed twice with PBS. Pellets are resuspended in 1 ml of cold PBS and added dropwise while gently vortexing to 9 ml 70 % ethanol in a 15 ml polypropylene centrifuge tube. Fixed cells are then frozen at –20 ℃ overnight. The next day, cells are centrifuged at 500 × g for 10 minutes at 4 ℃ and washed twice with 3 ml of cold PBS. Cells are resuspended in 400 μl of propidium iodide staining solution (0.2 mg/ml RNAse A, 0.02 mg/ml propidium iodide, 0.1 % Triton-X in PBS) and incubated for 15 minutes at 37 ℃.
In Vivo
In vivo

In three disseminated NMC xenograft models, NEO2734 provides greater growth inhibition, with tumor regression and significant survival benefit seen in two of three models, compared with a lead clinical BET inhibitor or “standard” chemotherapy.[1]
Animal Research Animal Models tumor bearing NSG mice
Dosages 8 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 435.44 Formula

C22H24F3N3O3
CAS No. 2081072-29-7 SDF --
Smiles CN1C=C(C=C(C)C1=O)C2=CC=C3N=C(C4CCOCC4)[N](CCOC(F)(F)F)C3=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (199.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble


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In vivo
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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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