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WIKI4

Cat. No. M4829
WIKI4 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 75  USD75 In stock
5mg USD 65  USD65 In stock
10mg USD 100  USD100 In stock
25mg USD 200  USD200 In stock
50mg USD 350  USD350 In stock
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Quality Control
Biological Activity

WIKI4 inhibits expression of ß-catenin target genes and cellular responses to Wnt/ß-catenin signaling in cancer cell lines as well as in human embryonic stem cells.Furthermore WIKI4 mediates its effects on Wnt/ß-catenin signaling by inhibiting the enzymatic activity of TNKS2, a regulator of AXIN ubiquitylation and degradation. While TNKS has previously been shown to be the target of small molecule inhibitors of Wnt/ß-catenin signaling, WIKI4 is structurally distinct from previously identified TNKS inhibitors.WIKI4 is a high potency tankyrase inhibitor and that it selectively inhibits tankyrases over other ARTD enzymes tested.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 521.59
Formula C29H23N5O3S
CAS Number 838818-26-1
Purity 99.83%
Solubility DMSO
Storage at -20°C
References

[1] Haikarainen T, et al. PLoS One. Structural basis and selectivity of tankyrase inhibition by a Wnt signaling inhibitor WIKI4.

[2] James RG, et al. PLoS One. WIKI4, a novel inhibitor of tankyrase and Wnt/ß-catenin signaling.

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Keywords: WIKI4 supplier, Wnt/beta-catenin, inhibitors

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