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TNKS-2-IN-1

Name: TNKS-2-IN-1
Brand: TargetMol
SKU: T77675
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T77675Cas No. 4765-59-7

TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.

TNKS-2-IN-1

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Purity: 98.34%

Catalog No. T77675Cas No. 4765-59-7

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$29	-	In Stock
25 mg	$30	-	In Stock
50 mg	$41	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.34%

Appearance:Solid

Color:Yellow

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Product Introduction

TNKS-2-IN-1 AI Summary

TNKS-2-IN-1 exhibits a range of bioactivities and potential pharmacological properties. It demonstrates antiproliferative activity against several human cancer cell lines, including K562, COLO205, and MDA-MB-231, with varying IC50 values. Additionally, it shows cytotoxicity against PC3 cells with an IC50 value exceeding 30,000 nM and against HT-29 cells without significant inhibition. The compound is also an inhibitor of multiple enzymes: human tankyrase2 at 10 nM with a 2.0% inhibition rate, beta-glucuronidase with an IC50 of 20,100 nM, and Saccharomyces cerevisiae alpha-glucosidase with an IC50 of 20,000 nM. Furthermore, it inhibits cytochrome P450 enzymes, particularly CYP1B1, with inhibition percentages from 71.5% to 91.9%, and shows moderate inhibition of CYP1A1 and CYP1A2. TNKS-2-IN-1 displays antibacterial activities against Escherichia coli and Staphylococcus aureus, although with MIC values greater than 128 μg/mL. It also inhibits E. coli MurA enzyme by 99.0% at 100 μM concentration. Additionally, it inhibits NLRP3 inflammasome activation in LPS-primed mouse J774A.1 cells with an IC50 of 5000 nM. Pharmacokinetic properties include a LogD7.4 of 2.5, an intrinsic clearance (CL) of 53.7 mL.min⁻¹.g⁻¹ in human liver microsomes, and a solubility of 1900 nM in pH 7.4 buffer. Despite its diverse bioactivities, it exhibits no inhibition of CDK4/Cyclin D1 at 10 μM. These biochemical and pharmacological properties indicate that TNKS-2-IN-1 could be a potential candidate for further drug development, though its specific applications and therapeutic indices require further elucidation..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.
Targets&IC50	TNKS1:259 nM, TNKS2:1100 nM

Chemical Properties

Molecular Weight	267.24
Formula	C₁₄H₉N₃O₃
Cas No.	4765-59-7
Smiles	[O-][N+](=O)c1ccc(cc1)-c1nc(=O)c2ccccc2[nH]1

Storage & Solubility Information

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Solubility Information	DMSO: < 1 mg/mL (insoluble or slightly soluble)

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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