IWR-1, also known as IWR-1-endo, is a an inhibitor of the Wnt signaling cascade through inhibiting TNKSs, binding only to the adenosine-binding site. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. IWR-1 inhibits cell proliferation and EMT even in the presence of TNF-α-induced cancer cell stimulation. IWR-1 also significantly suppressed cell migration, invasion, and matrix metalloproteinase activities of CRC cell lines. IWR-1 provides EMT reversal effects by directly suppressing survivin expression.
Chemical Formula: C25H19N3O3
Exact Mass: 409.1426
Molecular Weight: 409.44
Elemental Analysis: C, 73.34; H, 4.68; N, 10.26; O, 11.72
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects in vitro. IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly. IWR-1 (10 μM) induces stabilization of β-catenin disruption complex. IWR-1 (10 μM) is added to the medium together with MIF, the size of cell colonies is extremely decreased, and that indicates the promoting effect of MIF on NSPC proliferation is inhibited by IWR-1 in any MIF concentration group. 2, 5 and 10 μM of IWR-1 significantly inhibits the proliferation of NSPC dose-dependently. IWR-1 inhibites the promoting effect of MIF on NSPC differentiation to neuron lineage. IWR-1 treatment in the presence of maximal stimulatory dose of FSH (0.5 ng/mL) results in a dose dependent inhibition of the stimulatory effect of FSH with > 75% inhibition observed at the maximal inhibitory dose of IWR-1 (1 µM). IWR-1 treatment partially reverses the FSH-induced inhibition of granulosa cell CARTPT mRNA expression.
Lu J, et al. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7.
Zhang X, et al. Macrophage migration inhibitory factor promotes proliferation and neuronal differentiation of neural stem/precursor cells through Wnt/β-catenin signal pathway. Int J Biol Sci. 2013 Nov 28;9(10):1108-20.
Gupta PS, et al. Regulation and Regulatory Role of WNT Signaling in Potentiating FSH Action during Bovine Dominant Follicle Selection. PLoS One. 2014 Jun 17;9(6):e100201.
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