Structure of Wnt-C59
CAS No.: 1243243-89-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
8591-GSCs | 20 μM | 24 h | Inhibited invasion and migration | PMC6136228 |
8591-GSCs | 5 μM | 24 h | Inhibited invasion and migration | PMC6136228 |
U251-GSCs | 20 μM | 24 h | Inhibited invasion and migration | PMC6136228 |
U251-GSCs | 5 μM | 24 h | Inhibited invasion and migration | PMC6136228 |
ImMKCLs | 1.1 µM | 7 days | Promote MK maturation and PLP production | PMC6134216 |
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. | PMC4834146 |
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. | PMC4834146 |
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 | PMC4362247 |
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 | PMC4362247 |
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 | PMC4362247 |
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 | PMC4362247 |
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 | PMC4362247 |
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. | PMC7524370 |
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. | PMC9869633 |
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. | PMC4834146 |
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 | PMC6118584 |
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 | PMC4362247 |
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. | PMC7524370 |
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 | PMC6136228 |
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 | PMC6134216 |
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. | PMC10616556 |
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. | PMC10226545 |
Tags: Wnt-C59 | C59 | Wnt | Porcupine | tankyrase inhibitor | Wnt/β-catenin pathway | Wnt signaling | fibrosis | depletion of active β-catenin | stem cell maintenance | regenerative medicine | cancer | 1243243-89-1
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