1. Autophagy Metabolic Enzyme/Protease
  2. Autophagy Phosphatase
  3. SMIP-031

SMIP-031 is a potent and orally active PPM1A inhibitor with an IC50 value of 180 nM. SMIP-031 induces autophagy. SMIP-031 inhibits Mycobacterium tuberculosis infect in mice.

For research use only. We do not sell to patients.

SMIP-031 Chemical Structure

SMIP-031 Chemical Structure

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Description

SMIP-031 is a potent and orally active PPM1A inhibitor with an IC50 value of 180 nM. SMIP-031 induces autophagy. SMIP-031 inhibits Mycobacterium tuberculosis infect in mice[1].

IC50 & Target

IC50: 180 nM (PPM1A)[1]

In Vitro

SMIP-031 (0.5, 1, 2.5,5 µM; 5 days) reduces Mycobacterium tuberculosis (Mtb) burden in infected THP-1 cells in a dose-dependent manner[1].
SMIP-031 (0.25, 0.5, 1, 2, 4, 8 µM) induces autophagy by decreasing the protein expression of S403-p62 in Mtb-infected THP-1 macrophages[1].

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

Western Blot Analysis[1]

Cell Line: THP-1 macrophages (Mtb-infected)
Concentration: 0.25, 0.5, 1, 2, 4, 8 µM (bafilomycin 100 nM)
Incubation Time:
Result: Iecreased the protein expression of S403-p62 in a dose-dependent manner.
In Vivo

SMIP-031 (12.5, 50 mg/kg; i.p.; daily for 8 days) reduces the bacteria burden in vivo in the spleens of infected mice[1].
Pharmacokinetic Parameters (ICR (CD-1) mice; i.v. for 2 mg/kg; p.o. for 10 mg/kg)[1].

administration T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF-obs (h*ng/mL) CL obs (mL/min/kg) F (%)
p.o. 0.771 0.250 908 759 761 - 73.7
i.v. 0.634 - - 206 208 >170 -

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

Animal Model: BALB/c mice (Mtb mc26206 strain)[1]
Dosage: 12.5, 50 mg/kg
Administration: I.p.; daily for 14 days
Result: Reduced the Mtb burden and no weight loss or visible signs of toxicity were observed during the experiment.
Molecular Weight

366.22

Formula

C17H17BrFNO2

SMILES

OCC[N+]1=CC2=C(C=CC(OCC)=C2)C3=CC(F)=CC=C31.[Br-]

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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Help & FAQs
  • 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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Product Name:
SMIP-031
Cat. No.:
HY-163782
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