IWP-2 is an inhibitor ofWntprocessing and secretion with anIC₅₀of 27 nM. IWP-2 targets the membrane-bound O-acyltransferaseporcupine(Porcn) and thus preventing a crucialWntligand palmitoylation. IWP-2 is also an ATP-competitiveCK1δinhibitor with anIC₅₀of 40 nM for the gatekeeper mutant^M82FCK1δ^[1][2].

IWP-2 inhibits the proliferation of the investigated cell lines within the single digit μM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC₅₀s of 8.96 μM, 1.90 μM, 2.33 μM, 3.86 μM, 4.67 μM, 2.76 μM, 1.90 μM and 2.05 μM, respectively^[2].
Panc-1 cells are either untreated or treated with 2.33 μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells^[2].

To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the anti-inflammatory cytokine IL-10^[3].

466.60

Solid

C₂₂H₁₈N₄O₂S₃

686770-61-6

Room temperature in continental US; may vary elsewhere.

DMF : 12.5 mg/mL(26.79 mM;ultrasonic and warming and heat to 60℃)

DMSO : 2 mg/mL(4.29 mM;Need ultrasonic)

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