E722-2648|CAS 931963-55-2|DC Chemicals

Cas No.:	931963-55-2
Chemical Name:	N-[3-(3-Methyl-1-piperidinyl)propyl]-6,7,8,9-tetrahydro-1H-thiopyrano[4,3-B][1]benzothiophene-3-carboxamide
Synonyms:	N-[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]-
SMILES:	S1C2C=C(C(NCCCN3CCCC(C)C3)=O)SCC=2C2=C1CCCC2
Formula:	C₂₁H₃₀N₂Os₂
M.Wt:	390.605702877045
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	1. Helen Tanton, et al. Sci Adv. 2022 Apr 29;8(17):eabm3108.

Description:

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.

References:

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

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC70375	E722-2648	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.
DC46190	PRI-724	PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
DC40956	β-catenin-IN-2	β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.
DC29001	CWP232228	CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
DC10976	E-7386	E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin, disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 with IC50 of 55 and 73 nM, respectively.