1. Anti-infection
  2. Bacterial
  3. AX20017

AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.

For research use only. We do not sell to patients.

AX20017 Chemical Structure

AX20017 Chemical Structure

CAS No. : 329221-38-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 116 In-stock
Solution
10 mM * 1 mL in DMSO USD 116 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 84 In-stock
10 mg USD 120 In-stock
25 mg USD 252 In-stock
50 mg USD 432 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AX20017

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.

IC50 & Target

IC50: 0.39 μM (PknG)[1]

In Vitro

The compound AX20017 inhibitor is bound deep within a narrow pocket formed by the inter lobe cleft of the PknG domain. The main chain Glu233:O and Val235:NH of PknG form hydrogen bonds with AX20017[2].AX20017 results in mycobacterial transfer to lysosomes and killing of the mycobacteria. AX20017 does not affect the human kinases, whereas the activity of PknG is effectively inhibited. AX20017 does not affect cellular morphology, membrane ruffling, or macropinocytosis[3].

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

Molecular Weight

264.34

Formula

C13H16N2O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C1=C(NC(C2CC2)=O)SC3=C1CCCC3

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 : 130 mg/mL (491.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7830 mL 18.9150 mL 37.8301 mL
5 mM 0.7566 mL 3.7830 mL 7.5660 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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% Corn Oil

    Solubility: ≥ 3.25 mg/mL (12.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 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 (32.5 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)

g

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
References
Kinase Assay
[3]

In vitro phosphorylation by PknG (0.5 μg) is in 25 mM Tris (pH 7.5), 2 mM MnCl2, and 0.5 μCi [γ-32P]ATP in the absence or presence of the reagents. To monitor kinase activity of PknGΔN, the protein is combined with equal amounts of the kinase-dead mutant of full-length PknG, PknG-K181M. To analyze kinase activity of PknG-I87S/A92S and PknG-C/S, the PknG-N-terminal fragment of PknG (2 μg) is included. Phosphorylated proteins are separated on 12.5% SDS/PAGE and analyzed by autoradiography or quantitated by PhosphorImage analysis. IC50 values are determined by using a radiometric ATP consumptive assay. Twelve concentrations of AX20017 in the range from 5 × 10-5M to 1.5 × 10-10 M are tested in each kinase assay[3].

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

Cell Assay
[3]

Phagocytosis is analyzed after incubation of J774 cells for 30 min in the presence of the indicated concentration of AX20017 (0, 10, 20 μM), followed by incubating the cells for 2 h with latex beads at a ratio of 10:1 beads/cells in the continued presence of the inhibitor, followed by fixation in 3% paraformaldehyde as described. Cells are observed with a Axiophot using a ×63 objective. Proliferation of J774 cells is analyzed by incorporation of tritiated thymidine (0.1 μCi) for 12 h as described of cells that had been incubated for 48 h in the absence or presence of the AX20017(0, 10, 20 μM)[3].

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

References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7830 mL 18.9150 mL 37.8301 mL 94.5752 mL
5 mM 0.7566 mL 3.7830 mL 7.5660 mL 18.9150 mL
10 mM 0.3783 mL 1.8915 mL 3.7830 mL 9.4575 mL
15 mM 0.2522 mL 1.2610 mL 2.5220 mL 6.3050 mL
20 mM 0.1892 mL 0.9458 mL 1.8915 mL 4.7288 mL
25 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7830 mL
30 mM 0.1261 mL 0.6305 mL 1.2610 mL 3.1525 mL
40 mM 0.0946 mL 0.4729 mL 0.9458 mL 2.3644 mL
50 mM 0.0757 mL 0.3783 mL 0.7566 mL 1.8915 mL
60 mM 0.0631 mL 0.3153 mL 0.6305 mL 1.5763 mL
80 mM 0.0473 mL 0.2364 mL 0.4729 mL 1.1822 mL
100 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
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AX20017 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.

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AX20017
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