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  2. Bacterial
  3. AX20017

AX20017 

Cat. No.: HY-14987 Purity: 99.95%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
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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].

Molecular Weight

264.34

Formula

C₁₃H₁₆N₂O₂S

CAS No.

329221-38-7

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (121.06 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.3783 mL 1.8915 mL 3.7830 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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Keywords:

AX20017AX 20017AX-20017BacterialInhibitorinhibitorinhibit

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AX20017
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