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TH-257

Name: TH-257
Brand: TargetMol
SKU: T7128
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7128Cas No. 2244678-29-1

Alias TH 257

TH-257 is a Potent and selective allosteric LIMK 1/2 inhibitor(LIMK1 and LIMK2, IC50 of 84 nM and 39 nM).

TH-257

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Purity: 98.23%

Catalog No. T7128Alias TH 257Cas No. 2244678-29-1

TH-257 is a Potent and selective allosteric LIMK 1/2 inhibitor(LIMK1 and LIMK2, IC50 of 84 nM and 39 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$35	In Stock	In Stock
10 mg	$56	In Stock	In Stock
25 mg	$109	In Stock	In Stock
50 mg	$153	In Stock	In Stock
100 mg	$213	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$40	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.23%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

TH-257 AI Summary

TH-257 exhibits a diverse range of bioactivities, impacting cell viability, protein stability, and enzyme inhibition. In cell viability assays involving HEK293T cells, human fibroblasts, and U2OS cells, TH-257 demonstrated both growth-inhibitory and growth-stimulatory effects. Thermal Shift Assay results indicate that the compound alters the thermal stability of specific protein domains differently, either increasing or decreasing their melting temperatures. Most notably, TH-257 effectively inhibits LIMK1 and LIMK2 enzymes with IC50 values ranging from 14.45 nM to 229.09 nM across various assays, and also shows binding affinity to these targets. It additionally downregulates the expression of MISP, CLASP1, and MAPRE2 in HeLa cells, and affects PAK-mediated phosphorylation of LIMK1 and LIMK2, and phosphorylation of cofilin serine 3 in SH-SY5Y cells. Despite its specific action on LIMK1 and LIMK2, the compound exhibits weak binding affinity (Kd > 10000.0 nM) to EGFR, LCK, SLK, and SYK. It holds high aqueous solubility at pH 7 and good microsomal stability in rat and human liver microsomes, indicating a potential for therapeutic application targeting LIMK1 and LIMK2 pathways..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	TH-257 is a Potent and selective allosteric LIMK 1/2 inhibitor(LIMK1 and LIMK2, IC50 of 84 nM and 39 nM).
Targets&IC50	LIMK1:84 nM, LIMK2:39 nM
Synonyms	TH 257

Chemical Properties

Molecular Weight	422.54
Formula	C₂₄H₂₆N₂O₃S
Cas No.	2244678-29-1
Smiles	CCCCN(Cc1ccccc1)C(=O)c1ccc(cc1)S(=O)(=O)Nc1ccccc1
Relative Density.	no data available

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: 250 mg/mL (591.66 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.83 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3666 mL	11.8332 mL	23.6664 mL	118.3320 mL
5 mM	0.4733 mL	2.3666 mL	4.7333 mL	23.6664 mL
10 mM	0.2367 mL	1.1833 mL	2.3666 mL	11.8332 mL
20 mM	0.1183 mL	0.5917 mL	1.1833 mL	5.9166 mL
50 mM	0.0473 mL	0.2367 mL	0.4733 mL	2.3666 mL
100 mM	0.0237 mL	0.1183 mL	0.2367 mL	1.1833 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc