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AX20017

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Chemical Structure| 329221-38-7 同义名 : -
CAS号 : 329221-38-7
货号 : A499106
分子式 : C13H16N2O2S
纯度 : 99%+
分子量 : 264.343
MDL号 : MFCD00785286
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 125 mg/mL(472.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM[3]. Inhibition of PknG by AX20017 reduces mycobacterial survival in in vitro latency models such as hypoxia, persisters, and nutrient starvation[4]. Inhibition of PknG with the highly selective low-molecular-weight inhibitor AX20017 results in mycobacterial transfer to lysosomes and killing of the mycobacteria. The structure of PknG-AX20017 further reveals that the inhibitor is buried deep within the adenosine-binding site, targeting an active conformation of the kinase domain[5]. The available drug molecules and the ligand AX20017 showed hydrogen bond interaction with the aminoacid residues Glu233 and Val235[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.78mL

0.76mL

0.38mL

18.91mL

3.78mL

1.89mL

37.83mL

7.57mL

3.78mL
参考文献

[1]Santhi N, Aishwarya S. Insights from the molecular docking of withanolide derivatives to the target protein PknG from Mycobacterium tuberculosis. Bioinformation. 2011;7(1):1-4.

[2]Walburger A, Koul A, et al. Protein kinase G from pathogenic mycobacteria promotes survival within macrophages. Science. 2004 Jun 18;304(5678):1800-4.

[3]Walburger A, Koul A, Ferrari G, Nguyen L, Prescianotto-Baschong C, Huygen K, Klebl B, Thompson C, Bacher G, Pieters J. Protein kinase G from pathogenic mycobacteria promotes survival within macrophages. Science. 2004 Jun 18;304(5678):1800-4

[4]Khan MZ, Nandicoori VK. Deletion of pknG Abates Reactivation of Latent Mycobacterium tuberculosis in Mice. Antimicrob Agents Chemother. 2021 Mar 18;65(4):e02095-20

[5]Scherr N, Honnappa S, Kunz G, Mueller P, Jayachandran R, Winkler F, Pieters J, Steinmetz MO. Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):12151-6

[6]Santhi N, Aishwarya S. Insights from the molecular docking of withanolide derivatives to the target protein PknG from Mycobacterium tuberculosis. Bioinformation. 2011;7(1):1-4