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Chemical Structure : K-476
Catalog No.: PC-22045Not For Human Use, Lab Use Only.
K-476 is a highly potent and selective tankyrase (TNKS1/2) inhibitor, potently inhibits Wnt/β-catenin pathway with IC50 of 110 nM in cell-based luciferase assays.
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K-476 is a highly potent and selective tankyrase (TNKS1/2) inhibitor, potently inhibits Wnt/β-catenin pathway with IC50 of 110 nM in cell-based luciferase assays.
K-476 binds to the ADP-ribose and the nicotinamide binding pockets of TNKS.
K-476 (1 uM) completely inhibits TNKS1 and TNKS2, does not inhibit other PARP family enzymes (PARP1, 2, 3, 6, 7, 8, 10, 11 and 12) by > 40%, even at 10 uM.
K-476 stabilizes Axin proteins and inhibits downstream genes in COLO 320DM cells.
K-476 exerts an antitumor effect in combination with anti-PD-L1 antibody, stabilizes Axin 1 protein in tumor.
K-476 upregulates the production of Ccl3 and Ccl4 in the tumor microenvironment (TME) and increases CD8+ T cells in tumors.
| M.Wt | 552.61 | |
| Formula | C31H29FN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kinosada H, et al. Am J Cancer Res. 2021 Jan 1;11(1):264-276.
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