Chemical Structure : K-476
CAS No.:
1650574-06-3
K-476
(K476, TNKS inhibitor 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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552.61
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Formula
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C31H29FN6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(3-{[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]methyl}-2-oxo-3,4 dihydroquinazolin-1(2H)-yl)-2-fluorobenzonitrile
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References
1. Kinosada H, et al. Am J Cancer Res. 2021 Jan 1;11(1):264-276.
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