DC Chemicals · Product datasheet

E722-2648 — Datasheet

CAT. NO. DC70375

Product page and current package options

ParameterValue
Chemical NameN-[3-(3-Methyl-1-piperidinyl)propyl]-6,7,8,9-tetrahydro-1H-thiopyrano[4,3-B][1]benzothiophene-3-carboxamide
CAS No.931963-55-2
SynonymsN-[3-(3-methylpiperidin-1-yl)propyl]-6,7,8,9-tetrahydro-1H-thiopyrano[4,3-b][1]benzothiole-3-carboxamide;N-(3-(3-Methylpiperidin-1-yl)propyl)-6,7,8,9-tetrahydro-1H-benzo[4,5]thieno[3,2-c]thiopyran-3-carboxamide;GLXC-25824;AKOS001924701;CCG-169651;E-722-2648;E722-2648;931963-55-2;N-[3-(3-METHYL-1-PIPERIDINYL)PROPYL]-6,7,8,9-TETRAHYDRO-1H-THIOPYRANO[4,3-B][1]BENZOTHIOPHENE-3-CARBOXAMIDE;AKOS021616376;1H-Thiopyrano[4,3-b][1]benzothiophene-3-carboxamide, 6,7,8,9-tetrahydro-N-[3-(3-methyl-1-piperidinyl)propyl]-
FormulaC21H30N2OS2
M.Wt390.605702877045
SMILESS1C2C=C(C(NCCCN3CCCC(C)C3)=O)SCC=2C2=C1CCCC2
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

1. Helen Tanton, et al. Sci Adv. 2022 Apr 29;8(17):eabm3108.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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