Wnt-C59 (C59)

Description

Biological Activity

Protocol(Only for Reference)

Chemical Information

Cell Assay: ^[2]

Animal Study: ^[1]

References

貨號 Cat. No.: S7037
規格 Size: 5mgã€50 mg
品牌 Brand: Selleckchem

Wnt-C59 (C59)

Catalog No.S7037

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM.

Size

Price

Stock

Quantity

5mg	USD 311	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 1600	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	NMuMG (NMG) and MDA-MB 231 cells
Concentrations
Incubation Time	48 hours
Method	Seed cells at a concentration of 4×10³/well in 100 μL culture medium containing various amouts of Wnt-C59. Incubate cells for 48 hours at 37 â„ƒ. Add 10 μL/well cell proliferation reagent and incubate for 4 hours at 37 â„ƒ. Shake thoroughly for 1 min on a shaker. Measure the absorbance of the samples in a microplate (ELISA) reader.

Animal Models	Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors
Dosages	10 mg/kg
Administration	orally
Solubility	0.5% methylcellulose/0.2% Tween 80, 30 mg/mL

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 vitro

Wnt-C59 (C59) is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. Wnt-C59 (10 nM) blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. Wnt-C59 (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. Wnt-C59 (100 nM) inhibits the activity of all splice variants of murine PORCN in PORCN-null HT1080 cells transfected with PORCN. Wnt-C59 is a nanomolar inhibitor of mammalian PORCN acyltransferase activity and blocks activation of all evaluated human Wnts. Wnt-C59 does not significantly inhibit the proliferation of any of 46 tested cancer cell lines in vitro at concentrations that completely inhibit PORCN. ^[1] Wnt-C59 is capable to significantly inhibit proliferation and comparable to the ICG-001 treated NMuMG (NMG) cells. Wnt-C59 inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. Wnt-C59 inhibits proliferation of human MDA-MB 231 cells by >50%. ^[2] Wnt-C59 (a Porcupine inhibitor) blocks radiolabel incorporation of [¹²⁵I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine. ^[3]

Wnt-C59 concentration remains greater than 10-fold above the in vitro IC50 for at least 16 hours following a single oral dose (5 mg/kg) in mice. Wnt-C59 (10 mg/kg) prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. Wnt-C59 (10 mg/kg) decreases Wnt pathway activity and decreased proliferation in MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors as evident by decreased expression of β-catenin target gene expression. ^[1] Wnt-C59 (10%) topically administered 4 weeks decreases the size of dysplasia of SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice. ^[4]

Download Wnt-C59 (C59) SDF

Molecular Weight (MW)	379.45
Formula	C₂₅H₂₁N₃O
CAS No.	1243243-89-1

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	76 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	0.5% methylcellulose/0.2% Tween 80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.