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Wnt&Beta catenin

IWP-L6 (1427782-89-5)

IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 nM.IWP-L6, also known as PORCN Inhibitor III and Wnt Pathway Inhibitor XIX, is a potent inhibitor of PORCN (EC50 = 0.5 nM).

Not Intended for Therapeutic Use. For research use only.

CAS: 1427782-89-5 Category

IWP-L6 (1427782-89-5) Description

IWP-L6, also known as PORCN Inhibitor III and Wnt Pathway Inhibitor XIX, is a potent inhibitor of PORCN (EC50 = 0.5 nM). Porcupine is a member of the membrane-bound O-acyltransferase family of proteins. It catalyzes the palmitoylation of Wnt proteins, a process required for their secretion and activity.

Target: Porcupine in vitro: IWP-L6 effectively suppressed the phosphorylation of dishevelled 2 (Dvl2) in HEK293 cells, a biochemical event associated with many Wnt-dependent cellular responses. IWP-L6 inhibits Wnt mediated branching morphogenesis in cultured embryonic kidneys. in vivo: IWP-L6 is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity.

 

IWP-L6 (1427782-89-5) Specifications

Product Name IWP-L6
Synonyms IWP-L6; IWP L6; IWPL6; PORCN Inhibitor III; Wnt Pathway Inhibitor XIX.
Chemical Names N-(5-phenyl-2-pyridinyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1427782-89-5
Molecular Formula C25H20N4O2S2
Molecular Weight 472.581
Monoisotopic Mass 472.103 g/mol
MDL number N/A
InChIKey QESQGTFWEQMCMH-UHFFFAOYSA-N
InChi Code InChI=1S/C25H20N4O2S2/c30-22(28-21-12-11-18(15-26-21)17-7-3-1-4-8-17)16-33-25-27-20-13-14-32-23(20)24(31)29(25)19-9-5-2-6-10-19/h1-12,15H,13-14,16H2,(H,26,28,30)
SMILES O=C(NC1=NC=C(C2=CC=CC=C2)C=C1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5)=O
Form Powder
Color N/A
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application Potent PORCN inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • 1: You L, Zhang C, Yarravarapu N, Morlock L, Wang X, Zhang L, Williams NS, Lum L, Chen C. Development of a triazole class of highly potent Porcn inhibitors. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5891-5895. doi: 10.1016/j.bmcl.2016.11.012. Epub 2016 Nov 11. PubMed PMID: 27876319; PubMed Central PMCID: PMC5142825.
  • 2: Wang X, Moon J, Dodge ME, Pan X, Zhang L, Hanson JM, Tuladhar R, Ma Z, Shi H, Williams NS, Amatruda JF, Carroll TJ, Lum L, Chen C. The development of highly potent inhibitors for porcupine. J Med Chem. 2013 Mar 28;56(6):2700-4. doi: 10.1021/jm400159c. Epub 2013 Mar 19. PubMed PMID: 23477365; PubMed Central PMCID: PMC3631274.
  • 3: Gao X, Hannoush RN. Single-cell imaging of Wnt palmitoylation by theacyltransferase porcupine. Nat Chem Biol. 2014 Jan;10(1):61-8. doi: 10.1038/nchembio.1392. Epub 2013 Nov 24. PubMed PMID: 24292069.
  • Proffitt, K.D., Madan, B., Ke, Z., et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer Cancer Research 73(2), 502-507 (2013).

1 review for IWP-L6 (1427782-89-5)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The IWP-L6 (1427782-89-5) is high purity,also customer service is pretty nice !gotta try!!

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