CGP049090 Inhibitor CAS No. 35082-49-6

Cat. No.	Name	Size	Price	Add Cart
KI1252	CGP049090	5 mg	$500

Chemical Characteristic

Product Name	CGP049090
Synonyms	Cercosporin
CAS No.	35082-49-6
Molecular Weight	534.15
Formula	C₂₉H₂₆O₁₀
Smiles	O1COC2=CC(=O)c3c(c(c(c4c5C(=C(C(=O)c6c(cc1c(c2c34)c56)O)OC)CC(C)O)CC(C)O)OC)O
Chemical Structure

Biological activities

CGP049090 is a small molecule inhibitor of Wnt/β-catenin/lef-1 signaling. CGP049090 dose-dependently inhibits Tcf4/β-catenin interaction with an IC50 of 8.7 µM. ^[1] CGP049090 inhibits human heptaoma cell lines Hep40, HepG2 and Huh7 with IC50 of 0.74, 0.60 and 0.49 µM, respectively. CGP049090 causes apoptosis and cell cycle arrest in HepG2 and Huh7 cells. ^[2] CGP049090 efficiently kills CLL cells with a LC50 less than 1 µM, whereas normal B cells are not significantly affected. The LC50 values for CGP049090 are 0.12 and 0.42 µM in MEC-1 and JVM-3 cells, respectively. CGP049090 can induce apoptotic CLL cells death and apoptosis cleave lef-1 target genes. ^[3] CGP049090 inhibits growth of HCC xenografts in nude mice. ^[2] In vivo, 69% tumor is inhibited by CGP049090 when compared with vehicle-treated controls, and the intervention is well tolerated. ^[3]

Protocols

CGP049090 is dissolved completely in 70% DMSO in a stock concentration of 3.3 mM and stored in aliquots at -20 °C. ^[3]

References

[1] Lepourcelet M, et al. Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex. Cancer Cell. 2004, 5(1): 91-102. [2] Wei W, et al. Small molecule antagonists of Tcf4/beta-catenin complex inhibit the growth of HCC cells in vitro and in vivo. Int J Cancer. 2010, 126(10): 2426-2436. [3] Gandhirajan RK, et al. Small molecule inhibitors of Wnt/beta-catenin/lef-1 signaling induces apoptosis in chronic lymphocytic leukemia cells in vitro and in vivo. Neoplasia. 2010, 12(4): 326-335.

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