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Chemical Structure| 1243243-89-1 Chemical Structure| 1243243-89-1

Structure of Wnt-C59
CAS No.: 1243243-89-1

Chemical Structure| 1243243-89-1

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Wnt-C59 is a Wnt signaling pathway inhibitor with an IC50 value of 74 nM for Porcupine. Wnt-C59 has antitumor effects and can be used in research on Wnt-related cancers and regenerative medicine.

Synonyms: C59; PORCN Inhibitor II

4.5 *For Research Use Only !

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Product Details of Wnt-C59

CAS No. :1243243-89-1
Formula : C25H21N3O
M.W : 379.45
SMILES Code : O=C(NC1=CC=C(C2=CC=CN=C2)C=C1)CC3=CC=C(C4=CC(C)=NC=C4)C=C3
Synonyms :
C59; PORCN Inhibitor II
MDL No. :MFCD22201167
InChI Key :KHZOJCQBHJUJFY-UHFFFAOYSA-N
Pubchem ID :57519544

Safety of Wnt-C59

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary kidney fibroblasts 10 nM 24 h To study the effect of Wnt-C59 on TGF-β-induced Axin2 expression, results showed that Wnt-C59 significantly inhibited Axin2 expression. Kidney Int. 2016 May;89(5):1062-1074.
HK-2 cells 10 nM 24 h To study the effect of Wnt-C59 on TGF-β-induced Axin2 expression, results showed that Wnt-C59 significantly inhibited Axin2 expression. Kidney Int. 2016 May;89(5):1062-1074.
CC-SW-1 100 nM 10 days Inhibition of PORCN activity resulted in reduced cell number, indicating Wnt-C59 has an inhibitory effect on CC-SW-1 cells in vitro J Clin Invest. 2015 Mar 2;125(3):1269-85.
SNU-1196 100 nM 10 days Inhibition of PORCN activity resulted in reduced cell number, indicating Wnt-C59 has an inhibitory effect on SNU-1196 cells in vitro J Clin Invest. 2015 Mar 2;125(3):1269-85.
WITT-1 100 nM 10 days Inhibition of PORCN activity resulted in reduced cell number, indicating Wnt-C59 has an inhibitory effect on WITT-1 cells in vitro J Clin Invest. 2015 Mar 2;125(3):1269-85.
SNU-1079 100 nM 10 days Inhibition of PORCN activity resulted in reduced cell number, indicating Wnt-C59 has an inhibitory effect on SNU-1079 cells in vitro J Clin Invest. 2015 Mar 2;125(3):1269-85.
CC-LP-1 100 nM 10 days Inhibition of PORCN activity resulted in reduced cell number, indicating Wnt-C59 has an inhibitory effect on CC-LP-1 cells in vitro J Clin Invest. 2015 Mar 2;125(3):1269-85.
intestinal organoids 100 nM 24 h Wnt-C59 inhibited the protective effect of L. reuteri on intestinal organoids, leading to increased damage induced by C. rodentium, reduced expression of Wnt3, Lgr5, and R-spondin1, and inhibition of Paneth cell differentiation and antimicrobial peptide expression, accompanied by increased inflammatory cytokine expression. Gut Microbes. 2020 Jul 3;11(4):997-1014.
8591-GSCs 20 μM 24 h inhibited invasion and migration J Exp Clin Cancer Res. 2018 Sep 12;37(1):225.
8591-GSCs 5 μM 24 h inhibited invasion and migration J Exp Clin Cancer Res. 2018 Sep 12;37(1):225.
U251-GSCs 20 μM 24 h inhibited invasion and migration J Exp Clin Cancer Res. 2018 Sep 12;37(1):225.
U251-GSCs 5 μM 24 h inhibited invasion and migration J Exp Clin Cancer Res. 2018 Sep 12;37(1):225.
PM cells 5 μM 72 h WNT-C59 significantly reduced the growth stimulating effect of Meso-CAFs on PM cells in co-culture, but did not significantly affect PM cells alone. J Exp Clin Cancer Res. 2023 Jan 23;42(1):27.
imMKCLs 1.1 µM 7 days Promote MK maturation and PLP production Blood Adv. 2018 Sep 11;2(17):2262-2272.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Unilateral ureteral obstruction model Oral gavage 25 mg/kg Once daily for 7 days To study the effect of Wnt-C59 on renal fibrosis in the unilateral ureteral obstruction model, results showed that Wnt-C59 significantly attenuated kidney fibrosis and reduced collagen mRNA expression. Kidney Int. 2016 May;89(5):1062-1074.
Mice C57BL/6J mice Oral 100 mg/kg Single dose, sacrificed 24 hours later To examine the early effects of withdrawal of Wnt signaling in ISC proliferation, results showed a significant increase in proliferating cells in crypt base cells in the duodenum, jejunum, and ileum in C59-treated mice J Clin Invest. 2018 Aug 31;128(9):3806-3812
Rats Chemically induced cholangiocarcinoma model Intraperitoneal injection 20 mg/kg 3 times per week for 5 weeks Inhibition of the Wnt signaling pathway significantly reduced tumor size and number, indicating Wnt-C59 has therapeutic potential for cholangiocarcinoma in vivo J Clin Invest. 2015 Mar 2;125(3):1269-85.
Mice C. rodentium infection model Oral 5 mg/kg Once daily for 16 days Wnt-C59 reversed the protective effect of L. reuteri against C. rodentium infection, leading to increased weight loss, C. rodentium colonization, and pathological changes, reduced expression of Wnt3, Lgr5, and R-spondin1, and inhibition of Paneth cell differentiation and antimicrobial peptide expression, accompanied by increased inflammatory cytokine and LPS levels. Gut Microbes. 2020 Jul 3;11(4):997-1014.
BALB/c-nu mice Intracranial orthotopic xenograft model Oral administration 15 mg/kg Daily until the end of the experiment Inhibited tumor growth and prolonged survival time J Exp Clin Cancer Res. 2018 Sep 12;37(1):225.
C57BL/6JRj mice Anti-GPIbα antibody-induced thrombocytopenia model Intraperitoneal injection 100 mg/kg Once daily for 6 days Evaluate the effect of Wnt-C59 on promoting platelet recovery in vivo Blood Adv. 2018 Sep 11;2(17):2262-2272.
Mice Bile duct ligation model Intraperitoneal injection 30 mg/kg Once daily for 5 or 12 days Wnt-C59 significantly reduced the number of bile infarcts and inflammatory cells in the liver in the BDL model, suppressed the nuclear factor kappa B signaling pathway, and reduced cholestatic injury. Cell Mol Gastroenterol Hepatol. 2023;16(6):895-921
Mice DSS-induced colitis model Oral 10 mg/kg Once daily for 5 days Wnt-C59 was used to inhibit the Wnt signaling pathway to confirm that hucMSC-exo promotes mucosal healing by activating the Wnt/β-catenin pathway. The results showed that Wnt-C59 reversed the protective effects of hucMSC-exo in colitis mice, indicating that the efficacy of hucMSC-exo depends on the activation of the Wnt/β-catenin pathway. Int J Nanomedicine. 2023 May 25;18:2799-2818

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.35mL

5.27mL

2.64mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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