1. Anti-infection Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt
  2. Bacterial Phosphatase p38 MAPK ERK
  3. 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.

MptpB-IN-3

MptpB-IN-3 Chemical Structure

CAS No. : 3104354-58-4

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Description

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[1].

IC50 & Target[1]

ERK1

 

ERK2

 

In Vitro

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.

Western Blot Analysis[1]

Cell Line: IFN-γ-stimulated Raw264.7 cells overexpressing wild-type MptpB or catalytically inactive MptpB/C160S
Concentration: 5, 10 and 20 μM
Incubation Time: 1 h (preincubation); 2 h (IFN-γ stimulation)
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.
Parmacokinetics
Species Dose Route T1/2β C0 AUC0-t AUC0-∞ MRT0-t MRT0-∞ Vd CL Tmax Cmax Bioavailability
Mice[1] 50 mg/kg p.o. 1.88 h / 1889 ng·h/mL 2445 ng·h/mL 1.59 h 2.75 h / / 0.25 h 908 ng/mL 4.9 %
Mice[1] 5 mg/kg i.v. 3.75 h 51856 ng/mL 4753 ng·h/mL 4997 ng·h/mL 0.66 h 1.31 h 5377 mL/kg 1003 mL/h/kg / / /
In Vivo

MptpB-IN-3 (Compound 4) (5-50 mg/kg; p.o., i.v.; single dose) exhibits acceptable pharmacokinetic properties in male ICR mice, with an oral bioavailability of 4.9%[1].

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

Molecular Weight

536.55

Formula

C22H21FN4O7S2

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • 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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