Art. -Nr.: HY-12438

G007-LK

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

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

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Reinheit: 99.24%
CAS. Nr.: 1380672-07-0
Formel: C₂₅H₁₆ClN₇O₃S
Molecular Weight:529.96

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

G007-LK Chemical Structure

CAS. Nr.: 1380672-07-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target^[1]

TNKS2

25 nM (IC₅₀)

TNKS1

46 nM (IC₅₀)

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 320DM	GI₅₀	0.43 μM Compound: G007-LK	Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 30883102]
COLO 320DM	GI₅₀	1.5 μM Compound: G007-LK	Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay	[PMID: 30883102]
COLO 320DM	GI₅₀	0.43 μM Compound: 3; G007-LK	Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human COLO320DM cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 32202790]
COLO 320DM	GI₅₀	1.5 μM Compound: 3; G007-LK	Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay	[PMID: 32202790]
HEK293	IC₅₀	0.05 μM Compound: 66, G007-LK	Inhibition of TNKS1/2 in HEK293 cells assessed as inhibition of Wnt/beta-casein pathway after 24 hrs by luciferase reporter gene assay Inhibition of TNKS1/2 in HEK293 cells assessed as inhibition of Wnt/beta-casein pathway after 24 hrs by luciferase reporter gene assay	[PMID: 23473363]
HEK293	IC₅₀	4.5 nM Compound: G007-LK	Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay	[PMID: 30883102]
HEK293	IC₅₀	4.5 nM Compound: 3; G007-LK	Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay Inhibition of TNKS/TNKS2 (unknown origin) expressed in HEK293 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay	[PMID: 32202790]
RKO	GI₅₀	8.9 μM Compound: G007-LK	Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 30883102]
RKO	GI₅₀	8.9 μM Compound: 3; G007-LK	Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human RKO cells assessed inhibition of cell growth measured after 5 days by MTT assay	[PMID: 32202790]
Sf9	IC₅₀	>100000 nM Compound: G007-LK	Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS	[PMID: 30883102]
Sf9	IC₅₀	>100000 nM Compound: 3; G007-LK	Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS Inhibition of human recombinant N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in presence of biotinylated-NAD+ by ELIS	[PMID: 32202790]

In Vitro

G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC₅₀s of 46 nM and 25 nM, respectively, and a cellular IC₅₀ of 50 nM. G007-LK shows no inhibition of PARP1 at doses up to 20 μM, and has a high CYP3A4 inhibition IC₅₀ value (>25 μM)^[1]. G007-LK (0-20 μM) dose-dependently inhibits hepatocellular carcinoma (HCC) cell growth. G007-LK also downregulates the levels of YAP by upregulating AMOTL1 and AMOTL2 in HCC cell lines. In addition, G007-LK (0-20 μM) synergizes with MEK and AKT inhibitors to suppress HCC cell proliferation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

G007-LK displays great pharmacokinetic profile in ICR mice^[1]. G007-LK (100 mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5⁺ intestinal stem cells in mice. G007-LK (100 mg/kg chow, p.o.) specifically targets LGR5⁺ WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50 mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000 mg/kg chow, p.o) shows no effect on the alteration of duodenal morphology^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1380672-07-0
Appearance Solid
Molecular Weight 529.96
Formel C₂₅H₁₆ClN₇O₃S
Color Off-white to yellow
SMILES

ClC1=C(C=CC=C1)N2C(/C=C/C3=NN=C(C4=CC=C(C#N)C=C4)O3)=NN=C2C5=CC=C(S(C)(=O)=O)C=N5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

Cancer Discov

Distinct Colorectal Cancer-Associated APC Mutations Dictate Response to Tankyrase Inhibition. [Abstract]

2019 Oct;9(10):1358-1371. PMID: 31337618
EMBO Mol Med

Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance. [Abstract]

2023 Mar 8;15(3):e16235. PMID: 36652375
Int J Mol Sci

Wnt Signaling Inhibitors and Their Promising Role in Tumor Treatment. [Abstract]

2023 Apr 4;24(7):6733. PMID: 37047705
Lab Invest

Generation and characterization of a cell line from an intraductal tubulopapillary neoplasm of the pancreas. [Abstract]

2020 Jul;100(7):1003-1013. PMID: 32005909
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Am J Cancer Res

TNKS inhibitors potentiate proliferative inhibition of BET inhibitors via reducing β-Catenin in colorectal cancer cells. [Abstract]

2022 Mar 15;12(3):1069-1087. PMID: 35411247
Charité - Universitätsmedizin Berlin

2024 Feb 19.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 30 mg/mL (56.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8869 mL

9.4347 mL

18.8693 mL

5 mM

0.3774 mL

1.8869 mL

3.7739 mL

10 mM

0.1887 mL

0.9435 mL

1.8869 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (3.92 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[3]

For cell proliferation or apoptosis assays, SNU-449 and HLE cells are grown in a 5% CO₂ atmosphere, at 37°C, in RPMI Medium supplemented with 10% fetal bovine serum (FBS) and penicillin/streptomycin. HCC cells are treated with 0.1% DMSO, or 2.5 μM, 5 μM, 10 μM, 20μM XAV-939 or G007-LK, either alone or in combination with the MEK inhibitor U0126 (25 μM) or the AKT inhibitor MK-2206 (5 μM). Cell proliferation is analyzed using the BrdU Cell Proliferation Assay Kit, while apoptosis is assessed with the Cell Death Detection Elisa Plus Kit^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Drug treatment experiments are performed with wild type (wt), single or double transgenic Lgr5-EGFP-Ires-CreERT2;R26R-Confetti mice, unless indicated otherwise. G007-LK is administered orally either by gavage (10 or 50 mg/kg body mass once daily, vehicle: 15% dimethylsulfoxide [DMSO], 17.5% Cremophor EL, 8.75% Miglyol 810 N, 8.75% ethanol in phosphate buffered saline [PBS]) or in G007-LK enriched chow (100 or 1000 mg G007-LK/kg chow ad libitum, corresponding to a daily G007-LK dose of approximately 20 or 200 mg/kg body mass, respectively, for a mouse with a body mass of 25 g and consumption of approximately 5 g enriched diet/day). G007-LK treatments are initiated at the age of 5 weeks and 5 days for oral gavage treatment or 6 weeks for enriched chow administration and continued for 9 or 21 days, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Voronkov A, 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 Apr 11;56(7):3012-23. [Content Brief]

[2]. Norum JH, et al. The tankyrase inhibitor G007-LK inhibits small intestine LGR5+ stem cell proliferation without altering tissue morphology. Biol Res. 2018 Jan 9;51(1):3. [Content Brief]

[3]. Xin Chen, et al. Tankyrase inhibitors suppress hepatocellular carcinoma cell growth via modulating the Hippo cascade. PLoS One. 2017 Sep 6;12(9):e0184068. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8869 mL	9.4347 mL	18.8693 mL	47.1734 mL
	5 mM	0.3774 mL	1.8869 mL	3.7739 mL	9.4347 mL
	10 mM	0.1887 mL	0.9435 mL	1.8869 mL	4.7173 mL
	15 mM	0.1258 mL	0.6290 mL	1.2580 mL	3.1449 mL
	20 mM	0.0943 mL	0.4717 mL	0.9435 mL	2.3587 mL
	25 mM	0.0755 mL	0.3774 mL	0.7548 mL	1.8869 mL
	30 mM	0.0629 mL	0.3145 mL	0.6290 mL	1.5724 mL
	40 mM	0.0472 mL	0.2359 mL	0.4717 mL	1.1793 mL
	50 mM	0.0377 mL	0.1887 mL	0.3774 mL	0.9435 mL

Keywords

G007-LK

8 Cited Publications

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G007-LK

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) G007-LK

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

G007-LK

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) G007-LK

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

G007-LK Related Classifications

HY-12438 Related Classifications