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G007-LK

Catalog No. T6842 CAS 1380672-07-0

G007-LK is a selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.

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G007-LK, CAS 1380672-07-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 100.00
10 mg	In stock	$ 169.00
25 mg	In stock	$ 351.00
50 mg	In stock	$ 558.00
100 mg	In stock	$ 785.00
1 mL * 10 mM (in DMSO)	In stock	$ 125.00

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Purity: 98.62%

Purity: 98.17%

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Description	G007-LK is a selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
Targets&IC50	TNKS1:46 nM, TNKS2:25 nM
In vitro	G007-LK demonstrated anti-tumor efficacy in xenograft and genetically engineered CRC models. In the COLO-320DM model, it reduced levels of tankyrases 1 and 2, stabilized AXIN1 and AXIN2, and decreased β-catenin levels. G007-LK treatment increased the expression of KRT20 and TM4SF4 in COLO-320DM tumors. Administered at 20 mg/kg twice daily, G007-LK achieved a 61% inhibition of tumor growth. Additionally, it reduced Wnt/β-catenin signaling and cell proliferation in normal intestinal tissue.
In vivo	G007-LK inhibits Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thus promoting β-catenin destabilization. In cell culture, it completely blocks ligand-driven Wnt/β-catenin signaling and demonstrates inhibition of approximately 50% in APC mutation-driven signaling across most CRC cell lines. G007-LK reduces mitotic COLO-320DM cells from 24% to 12% and S-phase HCT-15 cells from 28% to 18% at a concentration of 0.2 μM. It also inhibits colony formation in CRC cell lines COLO-320DM and SW403. Furthermore, G007-LK suppresses organ growth with an IC50 of 80 nM.
Kinase Assay	TNKS1 and TNKS2 in vitro biochemical assays: G007-LK inhibitory activity at various doses (duplicates) is tested twice by TNKS1, TNSK2 Chemiluminescent Assay Kits, and the luminescence is measured.
Cell Research	Cell lines: APC-mutant CRC cell lines COLO-320DM. Concentrations: ~0.2 μM. Method: For colony formation assays,cells are seeded at 500 cells/well in 2 mL medium.Cell line in triplicate wells is treated with either 0.06% DMSO or compound in 0.06% DMSO and incubated for up to 17 days or until colonies became sufficiently large to quantify.Colonies are stained with 200 μL of 12 mM 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide to each well for 1 h,and colony numbers are quantitated with a GelCount scanner at 1200 dpi resolution.
Animal Research	Animal Models: Human APC –mutant CRC xenograft COLO-320DM. Formulation: 15% DMSO,17.5% Cremophor EL,8.75% ethanol,8.75% Miglyol 810N,50% PBS. Dosages: 20 mg/kg. Administration: intraperitoneal injection twice daily

Molecular Weight	529.96
Formula	C25H16ClN7O3S
CAS No.	1380672-07-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (175.5 mM)

References and Literature

1. Voronkov A, et al. J Med Chem, 2013, 56(7), 32012-3023. 2. Lau T, et al. Cancer Res, 2013, 73(10), 3132-3144.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Neural Regeneration Compound Library Neuronal Differentiation Compound Library Anti-Metabolism Disease Compound Library Anti-Breast Cancer Compound Library Osteogenesis Compound Library Anti-Ovarian Cancer Compound Library Anti-Prostate Cancer Compound Library Metabolism Compound Library Cytoskeletal Signaling Pathway Compound Library

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Keywords

G007-LK 1380672-07-0 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin G007LK Inhibitor poly ADP ribose polymerase G-007-LK G007 LK inhibit inhibitor

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