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Cat. No. Name Size Price Add Cart
KI1238PKF115-584QuoteQuote

Chemical Characteristic

Product NamePKF115-584
CAS No.121263-19-2
Molecular Weight 790.76
FormulaC44H38O14
Chemical Name(R)-1-(3,10-dihydroxy-12-((R)-2-(((4-hydroxyphenoxy)carbonyl)oxy)propyl)-2,6,7,11-tetramethoxy-4,9-dioxo-4,9-dihydroperylen-1-yl)propan-2-yl benzoate
SmilesC(=O)(OC(CC1=C(C(=O)c2c(cc(c3c4c(cc(c5C(=O)C(=C(c(c45)c1c23)CC(C)OC(=O)c1ccccc1)OC)O)OC)OC)O)OC)C)Oc1ccc(cc1)O
Chemical Structure

Biological activities

PKF115??84 is a T cell factor/β-catenin antagonist. The IC50 of PKF115??84 is 168 and 170 nM against the metastatic melanoma cell lines SkMel28 and Mewo cell lines, respectively. In contrast, PKF115??84 inhibits 1205LU and 451LU with IC50 of 235 and 254 nM, respectively. PKF115??84 dose-dependently down-regulatesboth of β-catenin transcriptional activity and β-catenin expression. PKF115??84 inhibits cell viability comparable to the effects observed in the metastatic melanoma cell lines.[1]PKF115??84 dose-dependently suppresses the expression of the β-catenin target genes cyclin D1 and c-Myc. PKF115??84 dose-dependently inhibits β-catenin-dependent transcription and H295R proliferation, even in the presence of increased steroidogenic factor-1 levels.PKF115??84 reduces the percentage of H295R cells in S-phase and increased the percentage of apoptotic cells.PKF115??84 inhibits proliferation of the H295R human adrenocarcinoma cell line, which harbors the CTNNB1 S45P mutation along with a homozygous R72P polymorphism and a heterozygous F338L mutation in the TP53 gene.[2]PKF115-584 efficiently kills CLL cells, with a LC50 of <1 µM, but not normal B cells.PKF115-584 inhibits tumor inhibition by 57% JVM-3 xenograft model.[3]

Protocols

PKF115-584is dissolved completely in 70% DMSO in a stock concentration of 3.3 mM and stored in aliquots at -20 °C.[3]

References

[1] Sinnberg T, et al.β-Catenin signaling increases during melanoma progression and promotes tumor cell survival and chemoresistance.PLoS One. 2011, 6(8):e23429
[2] Doghman M,et al. The T cell factor/beta-catenin antagonist PKF115-584 inhibits proliferation of adrenocortical carcinoma cells.J ClinEndocrinolMetab. 2008, 93(8):3222-3225.
[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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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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