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Cat. No. Product Name CAS No. Information
PC-61323

Carnosic acid

3650-09-7

Carnosic acid (Carnosate) is a naturally occurring phenolic compound with antioxidant, anti-inflammatory and antimicrobial properties, inhibits the BCL9/β-catenin interaction with Ki of 3.3 uM; inhibits β-catenin-dependent transcription, and destabilizes oncogenic β-catenin in colon cancer cells; reduces the expression of Sox2 and the number of SOX2+ cells in MB sphere cultures.

PC-61288

Tegatrabetan

1227637-23-1

Tegatrabetan (BC-2059, BC2059, Tegavivint) is an orally bioavailable β-catenin antagonist that disrupts the binding of β-catenin to TBL1 and promotes β-catenin degradation, attenuates nuclear and cytoplasmic levels of β-catenin; reduces transcriptional activity of TCF4 and expression of its target genes, cyclin D1, c-MYC and survivin. BC treatment dose-dependently induced apoptosis of cultured and primary AML BPCs; significantly improves the median survival of immune-depleted mice engrafted with either cultured or primary AML BPCs.

Blood Cancer

Phase 1 Clinical

PC-70120

PRI-724

847591-62-2

PRI-724 (PRI724) is a potent, specific, second generation CBP/beta-catenin antagonist with IC50 of 150 nM, an isomer or enantiomer of ICG-001; binds specifically to the co-activator CBP, but not to p300; selectively induce apoptosis in colon carcinoma cells but not in normal colon cells, and exhibits antitumor activity in the mouse xenograft models of colon cancer.

Blood Cancer

Phase 2 Clinical

PC-70092

KYA-1797K

1956356-56-1

A derivative of KY1220 with improved inhibitory activity for Wnt/β-catenin signaling; dose-dependently decreases Wnt3a-CM-induced TOPflash reporter activation with IC50 of 0.75 uM; more effectively reduces the levels of both β-catenin and pan-Ras as well as the activities of ERK and Akt in SW480 cells; binds to Axin (Kd to WT axin-RGS=0.29 uM) and destabilizes b-catenin and Ras; inhibits growth of CRC cells with GI50 of 4-5 uM; suppresses the tumors induced by APC and KRAS mutations in tumor xenograft mice (25 mg/kg, i.p.).

PC-70091

KY-1220

292168-79-7

KY-1220 is a small molecule destabilizer of both β-catenin and Ras via inhibition of the Wnt/β-catenin pathway (IC50=2.1 uM); dose-dependently decreases Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells; reduces β-catenin and pan-Ras protein levels via polyubiquitin-dependent proteasomal degradation, consequently inhibits the activities of both ERK and Akt in various CRC cell lines; efficiently inhibits proliferation and transformation in HCT15, SW480, D-WT and D-MT CRC cells.

PC-35350

SKL2001

909089-13-0 SKL2001 is a specific small molecule activator (agonist) of the Wnt/β-catenin pathway, stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction; strongly activates β-catenin responsive transcription, upregulates TOPflash reporter activity without effect on the activity of FOPFlash with mutated β-catenin/Tcf-binding elements, as well as either NF-κB or p53 reporter activity; upregulates the expression of Axin2, inhibits N-terminal β-catenin phosphorylation without affecting GSK-3β activity; suppresses preadipocyte differentiation, the alternative mesenchymal differentiation pathway.
PC-35329

E-7386

1799824-08-0 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; exhibits anti-tumor activity in vitro tumor proliferation panel against 28 human tumor cell lines; modulates the expression of Wnt signaling pathway related genes including AXIN2 and other genes, significantly suppressed the number of polyposis in a dose dependent manner at the dose 8.5-50 mg/kg, also significantly changed the expressions of Wnt related genes in whisker follicle of ApcMin/+mice model.

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