G007-LK
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.
For research use only. We do not sell to patients.
- Purity: 99.24%
- CAS No.: 1380672-07-0
- Formula: C25H16ClN7O3S
- Molecular Weight:529.96
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Targeted Diversity Library
HY-L099
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) G007-LK
More- Cancer Discov. 2019 Oct;9(10):1358-1371. [Abstract]
- EMBO Mol Med. 2023 Mar 8;15(3):e16235. [Abstract]
- Int J Mol Sci. 2023 Apr 4;24(7):6733. [Abstract]
- Lab Invest. 2020 Jul;100(7):1003-1013. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Am J Cancer Res. 2022 Mar 15;12(3):1069-1087. [Abstract]
- Charité - Universitätsmedizin Berlin. 2024 Feb 19.
- Patent. US20180263995A1.
Biological Activity
|
TNKS2 25 nM (IC50) |
TNKS1 46 nM (IC50) |
|
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1380672-07-0
-
Appearance Solid
-
Molecular Weight 529.96
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
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
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)
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 -
-
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
Purity & Documentation
-
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)
-
Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
G007-LK Related Classifications
HY-12438 Related Classifications
Powered by Bioz