G007-LK

Name: G007-LK
Brand: MedChemExpress
SKU: HY-12438
Rating: 5.0 (8 reviews)

Cat. No.: HY-12438 Purity: 99.24%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

G007-LK Chemical Structure

CAS No. : 1380672-07-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 154	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 154	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 209	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1067	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

8 Publications Citing Use of MCE G007-LK

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View All PARP Isoform Specific Products:

View All Isoforms

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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	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: 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]
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]
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: 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]
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]
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]
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]
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]
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]

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.

Molecular Weight

529.96

Formula

C₂₅H₁₆ClN₇O₃S

CAS No.

1380672-07-0

Appearance

Solid

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.24%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (248 KB) HNMR (272 KB) LCMS (385 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]

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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

G007-LK1380672-07-0PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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G007-LK

Customer Review

G007-LK Related Antibodies

8 Publications Citing Use of MCE G007-LK

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

G007-LK Related Antibodies

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Complete Stock Solution Preparation Table

G007-LK Related Classifications

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