MptpB-IN-3
MptpB-IN-3 is a selective inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with an IC50 of 0.19 μM. MptpB-IN-3 blocks MptpB-mediated inhibition of the macrophage MAPK pathway and restores the phosphorylation levels of Erk1/2 and p38. MptpB-IN-3 exhibits direct anti-tuberculosis activity against Mycobacterium tuberculosis and reduces the Mycobacterium tuberculosis load in mouse macrophages. MptpB-IN-3 can be used for tuberculosis research.
For research use only. We do not sell to patients.
- CAS No.: 3104354-58-4
- Formula: C22H21FN4O7S2
- Molecular Weight:536.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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ERK1 |
ERK2 |
MptpB-IN-3 (Compound 4) inhibits purified recombinant human PTP1B with an IC50 of 65.61 μM, demonstrating 345-fold selectivity for Mycobacterium tuberculosis MptpB over the human phosphatase[1].
MptpB-IN-3 inhibits the growth of drug-sensitive Mycobacterium tuberculosis H37Rv with a MIC of 1.94 μg/mL[1].
MptpB-IN-3 inhibits the growth of multi-drug-resistant Mycobacterium tuberculosis strains 13946 and 14862 with MICs of 3.80 μg/mL and 4.60 μg/mL, respectively, but is inactive against a pretomanid-resistant strain (MIC >32 μg/mL)[1].
MptpB-IN-3 (0.26-64 μg/mL; 48 h) exhibits no cytotoxicity against Vero and J774A.1 macrophage cells (IC50 >64 μg/mL) and low cytotoxicity against HepG2 cells (IC50 = 55.92 μg/mL)[1].
MptpB-IN-3 (1-10 μg/mL) reduces Mycobacterium tuberculosis burden in infected J774A.1 macrophages in a dose-dependent manner, and exhibits greater potency than Rifampicin and PA-824 at equivalent doses[1].
MptpB-IN-3 (5-20 μM; 3 h) specifically restores Erk1/2 and p38 phosphorylation in IFN-γ-stimulated Raw264.7 cells overexpressing wild-type Mycobacterium tuberculosis MptpB, reversing MptpB-mediated suppression of the MAPK pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IFN-γ-stimulated Raw264.7 cells overexpressing wild-type MptpB or catalytically inactive MptpB/C160S
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Concentration:5, 10 and 20 μM
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Incubation Time:1 h (preincubation); 2 h (IFN-γ stimulation)
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Result:Restored phosphorylation of Erk1/2 and p38 in cells expressing wild-type MptpB, reversing MptpB-mediated suppression of the MAPK pathway; no notable changes were observed in vector-control or MptpB/C160S-expressing cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3104354-58-4
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Molecular Weight 536.55
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Formula C22H21FN4O7S2
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SMILES
CCCC[C@H](N1C(/C(SC1=S)=C/C2=CC(F)=C(C=C2)O[C@@H]3COC4=NC([N+]([O-])=O)=CN4C3)=O)C(O)=O
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- MptpB-IN-3
- 3104354-58-4
- Bacterial
- Phosphatase
- p38 MAPK
- ERK
- Mycobacterium tuberculosis protein tyrosine phosphatase B
- Mycobacterium tuberculosis H37Rv
- J774A.1 macrophage cells
- p38
- human PTP1B
- Mycobacterium tuberculosis
- Erk1/2
- mouse macrophages
- multi-drug-resistant Mycobacterium tuberculosis
- macrophage MAPK pathway
- Inhibitor
- inhibitor
- inhibit