C59 inhibits PORCN activity in vitro at nanomolar concentrations, as assessed by inhibition of Wnt palmitoylation, Wnt interaction with the carrier protein Wntless/WLS, Wnt secretion, and Wnt activation of β-catenin reporter activity . Wnt-C59 was used
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of porcupine O-acyltransferase
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells. A porcupine homolog - Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase
1.Ho SY, Keller TH. (2015) The use of porcupine inhibitors to target Wnt-driven cancers.. Bioorg Med Chem Lett, 25 (23):(5472-6). [PMID:26522946][10.1021/op500134e]
2.Kozielewicz P, Shekhani R, Moser S, Bowin CF, Wesslowski J, Davidson G, Schulte G. (2021) Quantitative Profiling of WNT-3A Binding to All Human Frizzled Paralogues in HEK293 Cells by NanoBiT/BRET Assessments.. ACS Pharmacol Transl Sci, 4 (3):(1235-1245). [PMID:34151213][10.1021/op500134e]
3.Arthofer E, Hot B, Petersen J, Strakova K, Jäger S, Grundmann M, Kostenis E, Gutkind JS, Schulte G. (2016) WNT Stimulation Dissociates a Frizzled 4 Inactive-State Complex with Gα12/13.. Mol Pharmacol, 90 (4):(447-59). [PMID:27458145][10.1021/op500134e]
4.Lin HK et al.. (2018) Caveolin-1 down-regulation is required for Wnt5a-Frizzled 2 signalling in Ha-RasV12 -induced cell transformation.. J Cell Mol Med, [PMID:29502342]
5.Lu W et al.. (2016) CXCL12/CXCR4 Axis Regulates Aggrecanase Activation and Cartilage Degradation in a Post-Traumatic Osteoarthritis Rat Model.. Int J Mol Sci, 17 (10):[PMID:27690009]
6.Willems L et al.. (2020) Differentiation of Human Cardiac Atrial Appendage Stem Cells into Adult Cardiomyocytes: A Role for the Wnt Pathway?. Int J Mol Sci, 21 (11):[PMID:32486259]
7.Valnohova J et al.. (2018) Functional dissection of the N-terminal extracellular domains of Frizzled 6 reveals their roles for receptor localization and Dishevelled recruitment.. J Biol Chem, 293 (46):(17875-17887). [PMID:30237173]
8.Takakura N et al.. (2019) Generation and characterization of Suncus murinus intestinal organoid: a useful tool for studying motilin secretion.. Cell Biol Int, [PMID:31293061]
9.Xian L et al.. (2017) HMGA1 amplifies Wnt signalling and expands the intestinal stem cell compartment and Paneth cell niche.. Nat Commun, 8 (15008). [PMID:28452345]
10.Marruecos L et al.. (2020) I?Ba deficiency imposes a fetal phenotype to intestinal stem cells.. EMBO Rep, 21 (6):(e49708). [PMID:32270911]
11.Zhou W et al.. (2020) miR-6838-5p Affects Cell Growth, Migration, and Invasion by Targeting GPRIN3 via the Wnt/ß-Catenin Signaling Pathway in Gastric Cancer.. Pathobiology, 87 (6):(327-337). [PMID:33254176]
12.Jobe NP et al.. (2021) Reduced WNT5A signaling in melanoma cells favors an amoeboid mode of invasion.. Mol Oncol, 15 (7):(1835-1848). [PMID:33969605]
13.Radaszkiewicz T et al.. (2021) RNF43 inhibits WNT5A-driven signaling and suppresses melanoma invasion and resistance to the targeted therapy.. Elife, 10 [PMID:34702444]
14.Shinkawa T et al.. (2022) Subtypes in pancreatic ductal adenocarcinoma based on niche factor dependency show distinct drug treatment responses.. J Exp Clin Cancer Res, 41 (89). [PMID:35272688]
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E1712139