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Porcn-IN-1

Catalog No. T4438   CAS 2036044-77-4
Synonyms: Porcupine-IN-1

Porcn-IN-1 (Porcupine-IN-1) is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Porcn-IN-1 Chemical Structure
Porcn-IN-1, CAS 2036044-77-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
5 mg In stock $ 122.00
10 mg In stock $ 198.00
25 mg In stock $ 346.00
50 mg In stock $ 516.00
100 mg In stock $ 736.00
1 mL * 10 mM (in DMSO) In stock $ 133.00
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Purity: 99.61%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Porcn-IN-1 (Porcupine-IN-1) is an effective porcupine inhibitor (IC50: 0.5±0.2 nM).
Targets&IC50 Porcupine:0.5 Nm
In vitro Porcupine, an enzyme, facilitates the attachment of palmitoleate to a serine residue within Wnt proteins, essential for their secretion. Porcupine-IN-1 exhibits potency comparable to the clinical compound LGK974 in a cell-based STF reporter gene assay and effectively inhibits the secretion of Wnt3A, thereby confirming its role as a porcupine inhibitor[1].
In vivo Porcupine-IN-1 exhibits moderate metabolic clearance in human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg), while demonstrating high clearance rates in mouse liver microsomes (109 mL/min/kg)[1].
Cell Research HEK293T cells are transfected with pLinbin-Wnt3A plasmid or vehicle control. The HEK293T cells are then treated with or without compounds (Porcupine-IN-1). Western Blot is used after 48 h to analyze both the cell lysis and culture medium[1].
Synonyms Porcupine-IN-1
Molecular Weight 410.44
Formula C25H19FN4O
CAS No. 2036044-77-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (243.64 mM)

TargetMolReferences and Literature

1. Xu Z, Xu X, O’Laoi R, et al. Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the ‘reversed’amide scaffold[J]. Bioorganic & medicinal chemistry, 2016, 24(22): 5861-5872.

TargetMolCitations

1. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 2. Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Anti-Aging Compound Library Stem Cell Differentiation Compound Library Bioactive Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets
ETC-159 GNF-6231 IWP L6 IWP-2 Wnt-C59 IWP-O1 LGK974

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Keywords

Porcn-IN-1 2036044-77-4 Stem Cells Porcupine inhibit PorcnIN1 Inhibitor Porcupine-IN-1 Porcn IN 1 inhibitor

 

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