E722-2648 

E722-2648 is an inhibitor targeting the BCL9 and β-catenin complex with antitumor activity. E722-2648 blocks complex formation by disrupting the interaction between the two proteins, thereby inhibiting β-catenin-mediated transcriptional activity and downregulating the expression of WNT target genes. E722-2648 effectively inhibits tumor growth in colon cancer xenograft models and colorectal cancer mouse models. E722-2648 can be used for the research of colon cancer and colorectal cancer^[1][2].

E722-2648 (1-20 μM; 16 h) dose-dependently inhibits the formation of endogenous β-catenin/BCL9 complexes in Colo320 and HCT116 colorectal cancer cells, without disrupting the interaction between β-catenin and E-cadherin, and exhibits excellent target specificity^[1].
E722-2648 (6.25-25 μM; 16 h) dose-dependently inhibits the transcriptional activity of the Wnt/β-catenin pathway in dual-luciferase reporter assays using Colo320 and HCT116 colorectal cancer cells^[1].
E722-2648 (10 μM, 20 μM; 6-48 h) downregulates the mRNA expression levels of Wnt pathway target genes AXIN2 and CD44 in a time- and dose-dependent manner in Colo320 and HCT116 colorectal cancer cells^[1].
E722-2648 (25-50 μM; 24 h) dose-dependently downregulates the mRNA expression levels of Wnt pathway target genes AXIN2, CD44, and LGR5 in human neoplastic colon organoids carrying the APC gene c.4778delA mutation^[1].
E722-2648 (5-20 μM; 24-48 h) dose-dependently downregulates the protein expression levels of AXIN2, CD44 and active β-catenin, and simultaneously increases the level of cleaved PARP to induce apoptosis in Colo320 and HCT116 colorectal cancer cells, whereas it exerts no such effects on β-catenin-independent RKO cells^[1].
E722-2648 (20 μM; 48 h) significantly reduces the viability of HCT116 and Colo320 colorectal cancer cells. The decrease in cell viability becomes more pronounced when combined with the Wnt inhibitor ICG-001, the cholesterol synthesis inhibitor Lovastatin (HY-N0504), and the cholesterol esterification inhibitor Avasimibe (HY-13215). Exogenous cholesterol supplementation partially rescues the reduction in cell viability induced by E722-2648 treatment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

E722-2648 (4 mg/kg; i.p.; administered once every other day for 20 days) significantly reduces the weight and volume of intraperitoneal tumors in mice, exerting potent in vivo anti-colorectal cancer activity in a mouse intraperitoneal xenograft model of colorectal cancer established with HCT116 cells^[1].
E722-2648 (3 mg/kg; intratumoral injection; administered once every other day for 20 days) significantly inhibits subcutaneous tumor growth, reduces tumor weight and GFP fluorescence signals in tumor tissues, downregulates the expression of Wnt pathway target genes AXIN2 and CD44 in tumor tissues, suppresses tumor cell proliferation and tumor angiogenesis, induces tumor cell apoptosis, and decreases the infiltration of pro-tumor M2-like tumor-associated macrophages in the subcutaneous colorectal cancer xenograft model of NCr nude mice bearing HCT116-GFP cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

390.61

C₂₁H₃₀N₂OS₂

931963-55-2

O=C(C1=CC(SC2=C3CCCC2)=C3CS1)NCCCN4CCCC(C4)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Groenewald W, et al. The Role of WNT Pathway Mutations in Cancer Development and an Overview of Therapeutic Options. Cells. 2023;12(7):990. Published 2023 Mar 24.  [Content Brief]

  [2]. Cao M, et al. Classical Angiogenic Signaling Pathways and Novel Anti-Angiogenic Strategies for Colorectal Cancer. Curr Issues Mol Biol. 2022;44(10):4447-4471. Published 2022 Sep 26.  [Content Brief]