1. Stem Cell/Wnt
  2. Porcupine

Porcupine-IN-1 

Cat. No.: HY-111472 Purity: 99.08%
Handling Instructions

Porcupine-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.

For research use only. We do not sell to patients.

Porcupine-IN-1 Chemical Structure

Porcupine-IN-1 Chemical Structure

CAS No. : 2036044-77-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 298 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Porcupine-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.

IC50 & Target

IC50: 0.5±0.2 nM (Porcupine inhibitor)[1]

In Vitro

Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Porcupine-IN-1 is as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Porcupine-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor[1].

In Vivo

Porcupine-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg)[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (243.64 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4364 mL 12.1820 mL 24.3641 mL
5 mM 0.4873 mL 2.4364 mL 4.8728 mL
10 mM 0.2436 mL 1.2182 mL 2.4364 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

410.44

Formula

C₂₅H₁₉FN₄O

CAS No.

2036044-77-4

SMILES

FC1=C(C2=CC(C)=NC=C2)N=CC(CNC(C3=CC=C(C(C=CC=C4)=C4N5)C5=C3)=O)=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Porcupine-IN-1
Cat. No.:
HY-111472
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Porcupine-IN-1

Cat. No.: HY-111472