2018300-62-2

2018300-62-2 structure

Name: TPOP146
Chemical Name: TPOP146
CAS Number: 2018300-62-2
Molecular Formula: C₂₇H₃₅N₃O₅
Molecular Weight: 481.584
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-01-21 00:31:35
Modify Date: 2024-01-05 20:23:54
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

Name	TPOP146
Synonyms	1,4-Benzoxazepine-9-carboxamide, 7-(3,5-dimethoxyphenyl)-2,3,4,5-tetrahydro-N-[(3S)-1-methyl-3-piperidinyl]-4-(1-oxopropyl)- 7-(3,5-Dimethoxyphenyl)-N-[(3S)-1-methyl-3-piperidinyl]-4-propionyl-2,3,4,5-tetrahydro-1,4-benzoxazepine-9-carboxamide

Description	TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Signaling Pathways >> Epigenetics >> Histone Acetyltransferase Research Areas >> Cancer
Target	IC50: 134 nM (CBP); 5.02 μM (BRD4)[1]
In Vitro	Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments[1].
Kinase Assay	Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a final concentration of 2 μM in 20 μL volume. Compounds (TPOP146) are added at a final concentration of 10 μM. SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a dilution of 1:1000. Excitation and emission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature is raised with a step of 3°C per minute from 25 to 96°C, and fluorescence readings are taken at each interval[1].
References	[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.