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HA-100

Name: HA-100
Brand: TargetMol
SKU: T7648
Price: 57 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7648Cas No. 84468-24-6

HA-100 is an inhibitor of protein kinase

HA-100

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Purity: 99.44%

Catalog No. T7648Cas No. 84468-24-6

HA-100 is an inhibitor of protein kinase

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$57	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$217	In Stock	In Stock
50 mg	$389	In Stock	In Stock
100 mg	$569	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$63	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:99.44%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

HA-100 AI Summary

HA-100 exhibits significant pharmacological activity across various biological targets. It demonstrates a binding affinity to the human adenosine A3 receptor in HEK293 cells with a Ki value of 25000.0 nM. This compound also acts as an inhibitor of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA) with IC50 values of 12000.0 nM and 6000.0 nM, respectively. Additionally, it shows antimalarial activity against drug-resistant Plasmodium falciparum strains D6 and W2 with IC50 values greater than 36000.0 nM and 4300.0 nM, respectively. Further bioactivity assays reveal that HA-100 inhibits Human Jumonji Domain Containing 2E (JMJD2E) with a potency of 39810.7 nM, and Cytochrome P450 2C19 (CYP2C19) with a potency of 10000.0 nM. It also functions as both an activator and inhibitor/substrate of Cytochrome P450 3A4 (CYP3A4) with potencies of 12589.3 nM. Moreover, it modulates lipid storage with a potency of 15848.9 nM, and inhibitis human tyrosyl-DNA phosphodiesterase 1 (TDP1) with potencies of 29855.4 nM and 33498.3 nM in the absence and presence of CPT, respectively. In antiviral assays, HA-100 inhibits SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells, though the inhibition percentages are relatively low at -4.72% and 0.17% at a concentration of 10 µM after 48 hours. Moreover, it shows 12.96% inhibition of the SARS-CoV-2 3CL-Pro protease at a concentration of 20 µM using a FRET-based assay with a peptide substrate. Finally, HA-100 shows 15.11% inhibition of human HDAC6 in an enzymatic assay using a commercial peptide substrate, but exhibits -3.91% inhibition in a similar assay using a custom peptide substrate..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	HA-100 is an inhibitor of protein kinase
Targets&IC50	PKG:4 μM , PKC:12 μM, PKC:6.5 μM (Ki), PKA:8 μM , MLCK:240 μM , MLCK:61 μM (Ki)

Chemical Properties

Molecular Weight	277.34
Formula	C₁₃H₁₅N₃O₂S
Cas No.	84468-24-6
Smiles	O=S(=O)(N1CCNCC1)c1cccc2cnccc12
Relative Density.	1.332 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 150 mg/mL (540.85 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (14.42 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	3.6057 mL	18.0284 mL	36.0568 mL	180.2841 mL
5 mM	0.7211 mL	3.6057 mL	7.2114 mL	36.0568 mL
10 mM	0.3606 mL	1.8028 mL	3.6057 mL	18.0284 mL
20 mM	0.1803 mL	0.9014 mL	1.8028 mL	9.0142 mL
50 mM	0.0721 mL	0.3606 mL	0.7211 mL	3.6057 mL
100 mM	0.0361 mL	0.1803 mL	0.3606 mL	1.8028 mL

Calculator

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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