TPOP146( TPOP-146 | TPOP 146 )

Catalog No. M13144 CAS No. 2018300-62-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

TPOP146
Note

Research use only, not for human use.
Brief Description

A potent and selective CBP/p300 bromodomain inhibitor with Kd of 134 nM for CBP bromodomain.
Description

A potent and selective CBP/p300 bromodomain inhibitor with Kd of 134 nM for CBP bromodomain, displays excellent selectivity over other bromodomains (>30-fold over BRD4 (1)); targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments.
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. They are for reference only.
In Vivo

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Synonyms

TPOP-146 | TPOP 146
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

2018300-62-2
Formula Weight

481.5839
Molecular Formula

C27H35N3O5
Purity

>98% (HPLC)
Solubility

DMSO
SMILES

COC1=CC(C2=CC(C(N[C@H]3CCCN(C)C3)=O)=C(OCCN(C(CC)=O)C4)C4=C2)=CC(OC)=C1
Chemical Name

1,4-Benzoxazepine-9-carboxamide, 7-(3,5-dimethoxyphenyl)-2,3,4,5-tetrahydro-N-[(3S)-1-methyl-3-piperidinyl]-4-(1-oxopropyl)-

1. Popp TA, et al. J Med Chem. 2016 Oct 13;59(19):8889-8912.

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