Description
IC50: 27 nM IWP-2-V2 is a Wnt production inhibitor. Wnt signaling proteins are small secreted proteins that are active in tissue homeostasis, embryonic development, and tumorigenesis. Wnt proteins bind to receptors, initiating a signaling cascade that results in β-catenin activation of gene transcription. In vitro: IWP-2 was identified as an inhibitor of Wnt production inactivating porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity was essential for the signaling ability and secretion of Wnt proteins. IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound. IWP-2-V2 was used to evaluate which structural features of IWP-2 were critical for impairing Wnt/β-catenin pathway activity . In vivo: In CCI rats, repetitive i.t. administration of IWP-2 (20 μM) in the early phase could significantly delay production of mechanical allodynia. The same drug administrated in the late phase produced long-lasting inhibitory effects on the established mechanical allodynia. Such analgesia lasted 4–6 days for IWP-2 after termination of the third treatment. These results showed similar inhibitory effects of IWP-2 on thermal hyperalgesia after CCI treatment . Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 877618-79-6
Molecular Weight: 480.63
Formula: C23H20N4O2S3
Chemical Name: 2-({3-benzyl-4-oxo-3H,4H,6H,7H-thieno[3,2-d]pyrimidin-2-yl}sulfanyl)-N-(6-methyl-1,3-benzothiazol-2-yl)acetamide
Smiles: CC1C=CC2N=C(NC(=O)CSC3=NC4CCSC=4C(=O)N3CC3C=CC=CC=3)SC=2C=1
InChiKey: VBUSMYOJWTVVPF-UHFFFAOYSA-N
InChi: InChI=1S/C23H20N4O2S3/c1-14-7-8-16-18(11-14)32-22(24-16)26-19(28)13-31-23-25-17-9-10-30-20(17)21(29)27(23)12-15-5-3-2-4-6-15/h2-8,11H,9-10,12-13H2,1H3,(H,24,26,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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