A chemical probe for the bromodomains of CECR2 and BPTF
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TP-238 (hydrochloride)

Item No. 27254

Technical Information
Formal Name
6-[4-[3-(dimethylamino)propoxy]phenyl]-2-(methylsulfonyl)-N-[3-(1H-pyrazol-1-yl)propyl]-4-pyrimidinamine, monohydrochloride
CAS Number
2415263-05-5
Molecular Formula
C22H30N6O3S • HCl
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMSO: 1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
272 nm
SMILES
CN(C)CCCOC1=CC=C(C2=NC(S(C)(=O)=O)=NC(NCCCN3N=CC=C3)=C2)C=C1.Cl
InChi Code
InChI=1S/C22H30N6O3S.ClH/c1-27(2)13-6-16-31-19-9-7-18(8-10-19)20-17-21(26-22(25-20)32(3,29)30)23-11-4-14-28-15-5-12-24-28;/h5,7-10,12,15,17H,4,6,11,13-14,16H2,1-3H3,(H,23,25,26);1H
InChi Key
FHVADRKEPFRFFF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    TP-238 is a chemical probe for the bromodomains of cat eye syndrome chromosome region, candidate 2 (CECR2) and bromodomain PHD finger transcription factor (BPTF). It has on-target biochemical activity with CECR2 when used at concentrations ranging from 10 to 30 nM and with BPTF at concentrations ranging from 100 to 350 nM. It is selective for the CECR2 and BPTF bromodomains over BRD9 (IC50 = 1.4 µM), as well as over a panel of 338 kinases at 1 µM. TP-238 binds to CECR2 and BPTF with KD values of 10 and 120 nM, respectively, in an isothermal titration calorimetry (ITC) assay and IC50 values of 30 and 350 nM, respectively, in an AlphaScreen® assay. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.