G007-LK (Synonyms: Tankyrase 1/2 Inhibitor VI) |
| Catalog No.GC13541 |
G007-LK est un inhibiteur puissant et sélectif de TNKS1 et TNKS2, avec des IC50 de 46 nM et 25 nM, respectivement.
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Cas No.: 1380672-07-0
Sample solution is provided at 25 µL, 10mM.
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G007-LK is a potent and specific inhibitor of tankyrase 1/2 with IC50 values of 46 and 25 nM [1].
The telomeric repeat factor 1 (TRF1)-interacting ankyrin-related ADP-ribose polymerase 1 (tankyrase 1,TNKS1) and tankyrase 2 (TNKS2) belong to the subgroup of poly(ADP-ribosyl)ating polymerases and regulate the assembly and disassembly of large polymerized structures [1].
G007-LK is a potent and specific tankyrase 1/2 inhibitor. G007-LK reduced auto-poly-(ADP ribosy)lation of TNKS1 and TNKS2 with IC50 values of 46 nM and 25 nM, respectively. In Wnt3a-induced HEK 293 cells, G007-LK inhibited ST-Luc with IC50 value of 0.05 μM [1]. In SW480 colorectal cancer cell line transfected with GFP-TNKS1, G007-LK induces highly dynamic and mobile degradasomes containing phosphorylated beta-catenin, beta-TrCP and ubiquitin [2]. In the APC-mutant cell lines, G007-LK reduces cytosolic and nuclear β-catenin protein levels [3].
In mice bearing COLO-320DM cell xenografts, G007-LK (20 mg/kg twice daily or 40 mg/kg daily) concentration-dependently inhibited tumor growth by 61% and 48%, respectively. Also, G007-LK reduced the levels of TNKS1/2 and β-catenin, and stabilized AXIN1/2 [3].
References:
[1]. Voronkov A, Holsworth DD, Waaler J, et al. Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor. J Med Chem, 2013, 56(7): 3012-3023.
[2]. Thorvaldsen TE, Pedersen NM, Wenzel EM, et al. Structure, Dynamics and Functionality of Tankyrase Inhibitor-induced Degradasomes. Mol Cancer Res, 2015, pii: molcanres.0125.2015.
[3]. Lau T, Chan E, Callow M, et al. A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth. Cancer Res, 2013, 73(10): 3132-3144.
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