HC102A
HC102A is an Antibacterial agent and an inhibitor of DosS and DosT histidine sensor kinases, with an IC50 of 1.9 μM against Mycobacterium tuberculosis DosS. HC102A does not alter the heme redox state of sensor kinases. HC102A reduces triacylglycerol synthesis and accumulation, decreases the survival rate of Mtb under non-replicating persistent and hypoxic conditions, and enhances the sensitivity of Mtb to Isoniazid (HY-B0329). HC102A can be used in research related to tuberculosis.
For research use only. We do not sell to patients.
- CAS No.: 91216-38-5
- Formula: C11H18N2O2
- Molecular Weight:210.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
HC102A (0.01-100 μM) potently and selectively inhibits DosR-dependent GFP fluorescence in Mtb CDC1551 (hspX′::GFP), with an EC50 of 12.4 μM[1].
HC102A (40 μM; 6 days) reduces TAG accumulation by 67% in Mtb CDC1551, thereby disrupting a key lipid metabolic process associated with persistence[1].
HC102A (1-100 μM; 10 days) reduces the survival rates of Mtb CDC1551 and Erdman strains in a dose-dependent manner under hypoxic NRP conditions, and decreases the strain survival rate by approximately 50% at a dose of 10 μM[1].
HC102A (1 h) directly inhibits autophosphorylation of purified Mtb DosS protein with an IC50 of 1.9 μM, but has minimal effect on autophosphorylation of DosT[1].
HC102A directly inhibits the autophosphorylation activity of the Mycobacterium tuberculosis DosS sensor kinase, but exerts no such effect on the DosT sensor kinase[2].
HC102A inhibits the autokinase activity of DosS and DosT histidine kinases in *Mycobacterium tuberculosis*, reduces the hypoxia-induced survival rate of *Mycobacterium tuberculosis*, and exhibits extremely low cytotoxicity against mammalian cell lines[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 91216-38-5
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Molecular Weight 210.28
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Formula C11H18N2O2
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SMILES
O=C1NC(=O)C2(N1)CC(C)CC(C)(C)C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Zheng H, et al. Inhibitors of Mycobacterium tuberculosis DosRST signaling and persistence. Nature chemical biology. 2017 Feb;13(2):218-225. [Content Brief]
[2]. Johnson BK, et al. Small Molecules That Sabotage Bacterial Virulence. Trends in pharmacological sciences. 2017 Apr;38(4):339-362. [Content Brief]
[3]. Stupar M, et al. Two-component sensor histidine kinases of Mycobacterium tuberculosis: Beacons for niche navigation. Molecular microbiology. 2022 May;117(5):973-985. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)