K-476 | TNKS1/2 inhibitor | Probechem Biochemicals

Chemical Structure : K-476

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K-476 (K476, TNKS inhibitor K-476)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	552.61
分子式	C31H29FN6O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(3-{[1-(6,7-dimethoxyquinazolin-4-yl)piperidin-4-yl]methyl}-2-oxo-3,4 dihydroquinazolin-1(2H)-yl)-2-fluorobenzonitrile

参考文献

1. Kinosada H, et al. Am J Cancer Res. 2021 Jan 1;11(1):264-276.

K-476 (K476, TNKS inhibitor K-476)

生物&药学活性

物理化学性质&存储条件

参考文献

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K-476 (K476, TNKS inhibitor K-476)

生物&药学活性

物理化学性质&存储条件

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