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ML281

Name: ML281
Brand: TargetMol
SKU: T3423
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3423Cas No. 1404437-62-2

ML281, a potent and selective STK33 inhibitor, exhibits an IC50 of 14 nM.

ML281

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Purity: 99.87%

Catalog No. T3423Cas No. 1404437-62-2

ML281, a potent and selective STK33 inhibitor, exhibits an IC50 of 14 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$73	In Stock	In Stock
10 mg	$98	In Stock	In Stock
25 mg	$198	In Stock	In Stock
50 mg	$328	In Stock	In Stock
100 mg	$526	-	In Stock
500 mg	$1,150	-	In Stock
1 mL x 10 mM (in DMSO)	$80	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:99.87%

Appearance:Solid

Color:White

Resource Download

COA LCMS HPLC HNMR

Product Introduction

ML281 AI Summary

ML281 exhibits significant bioactivity and selectivity features, comprising metabolic stability with degradation rates of 10.0% in mouse plasma and 80.3% in human plasma after 5 hours. It shows high plasma protein binding in both mouse (99.9%) and human (99.6%) plasma. The solubility of ML281 in PBS at pH 7.4 is 5800.0 nM. In terms of enzymatic inhibition, ML281 demonstrates potent inhibition of N-terminal 6His-tagged full-length human recombinant STK33 with an IC50 value of 14.0 nM, using myelin basic protein as substrate. It also inhibits human KDR and FLT3 at 1 µM, with inhibition percentages of ≥25.0% for each. The compound shows a high IC50 value (>10,000.0 nM) for inhibition of His-tagged recombinant catalytic fragment of PKA, translating to a selectivity ratio of IC50 for PKA to STK33 of >700.0. Additionally, it shows selectivity for STK33 over Aurora kinase B with a ratio IC50 of 550.0. Regarding its antiviral activity, ML281 inhibits SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 µM after 48 hours, showing 5.22% inhibition as determined by high content imaging. It also exhibits SARS-CoV-2 3CL-Pro protease inhibition activity with 6.1% and 31.01% inhibition at a concentration of 20 µM. However, its inhibition of SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10 µM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus shows minimal effects with percentages of 0.19% and -0.06% in different assays. Furthermore, ML281 shows significant inhibition of the human HDAC6 enzyme, particularly demonstrating 40.5% inhibition using a commercial peptide substrate and 4.16% inhibition using a custom peptide substrate..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	ML281, a potent and selective STK33 inhibitor, exhibits an IC50 of 14 nM.
Targets&IC50	STK33:14 nM.

Chemical Properties

Molecular Weight	389.47
Formula	C₂₂H₁₉N₃O₂S
Cas No.	1404437-62-2
Smiles	CC(C)c1ccc(NC(=O)c2cccs2)c(c1)-c1nc2ccccc2[nH]c1=O
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: 50 mg/mL (128.38 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5676 mL	12.8380 mL	25.6759 mL	128.3796 mL
5 mM	0.5135 mL	2.5676 mL	5.1352 mL	25.6759 mL
10 mM	0.2568 mL	1.2838 mL	2.5676 mL	12.8380 mL
20 mM	0.1284 mL	0.6419 mL	1.2838 mL	6.4190 mL
50 mM	0.0514 mL	0.2568 mL	0.5135 mL	2.5676 mL
100 mM	0.0257 mL	0.1284 mL	0.2568 mL	1.2838 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