2. Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein Stem Cell/Wnt
  3. Phosphodiesterase (PDE) p38 MAPK LPL Receptor ERK JNK
  4. Autotaxin-IN-8

Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis.

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

Autotaxin-IN-8

Autotaxin-IN-8 Chemical Structure

CAS No. : 3058084-21-9

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Autotaxin-IN-8 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

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ERK ERK1 ERK2 ERK5 ERK8

View All JNK Isoform Specific Products:

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JNK1 JNK2 JNK3 JNK

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Description

Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis[1].

IC50 & Target[1]

ERK1

 

ERK2

 

LPA1 Receptor

 

Autotaxin

14.2 nM (IC50)

In Vitro

Autotaxin-IN-8 (14.2 nM; 2 h) potently inhibits recombinant human ATX enzymatic activity with an in vitro IC50 of 14.2 nM[1].
Autotaxin-IN-8 (94.31 μM; 24 h) shows low cytotoxicity toward human normal lung epithelial L132 cells with an IC50 of 94.31 μM[1].
Autotaxin-IN-8 (1 μM; 12 h) significantly inhibits basal, TGF-β-stimulated, and LPC-stimulated migration of A549 cells over 12 h[1].
Autotaxin-IN-8 (1 μM; 48 h) significantly reduces spontaneous, TGF-β-triggered, and LPC-triggered collagen gel contraction by MLg cells over 48 h[1].

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

Autotaxin-IN-8 Related Antibodies

Western Blot Analysis[1]

Cell Line: Human normal lung epithelial L132 cells
Concentration: 0.1-5.0 μM (concentration-dependent study); 0.5 μM (time-dependent study); 0.5 μM (LPC/LPA co-treatment pre-incubation); 0.5 μM (TGF-β co-treatment pre-incubation)
Incubation Time: 75 min (concentration-dependent study); 30-75 min (time-dependent study); 75 min pre-incubation + 15 min LPC/LPA stimulation (co-treatment); 3 h pre-incubation + 3 h TGF-β stimulation (co-treatment)
Result: Inhibited phosphorylation of p-JNK with an EC50 of 0.958 μM, p-p38 with an EC50 of 0.785 μM, and p-ERK1/2 with an EC50 of 0.297 μM, with marked inhibition at concentrations as low as 0.5 μM.
Inhibited phosphorylation of p-JNK with an estimated time of 35.4 min, p-p38 with an estimated time of 39.13 min, and p-ERK1/2 with an estimated time of 30.46 min, with effects observed within 30 min.
Suppressed LPC-induced activation of p-JNK, p-p38, and p-ERK1/2 but had no effect on LPA-induced activation.
Significantly reduced TGF-β-induced phosphorylation of JNK, ERK, and p38.
Parmacokinetics
Species Dose Route Tmax Cmax T1/2 AUC0-last
Rat[1] 1 mg/kg p.o. 2.67 h 135.26 ng/mL 5.49 h 631.01
In Vivo

Autotaxin-IN-8 (1 mg/kg; p.o.; single dose) achieves up to 97% suppression of plasma LPA18:2, with >75% reduction sustained for 12 hours in female Wistar rats[1].
Autotaxin-IN-8 (1-3 mg/kg; p.o.; daily; 21 days) reduces collagen deposition, fibrosis marker expression, and inflammation in a Bleomycin (HY-17565A)-induced pulmonary fibrosis mouse model[1].

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

Animal Model: C57BL/6 (male, 8 weeks old, bleomycin-induced pulmonary fibrosis)[1]
Dosage: 1 mg/kg; 3 mg/kg
Administration: p.o.; daily; 21 days
Result: Markedly reduced bleomycin-induced collagen deposition in lung tissue.
Decreased lung tissue expression of α-SMA and TGF-β.
Suppressed the bleomycin-induced increase in LPAR1 and p-ERK1/2.
Mitigated bleomycin-provoked inflammatory responses by reducing IL-1β and IL-6 expression in lung tissue.
Molecular Weight

449.90

Formula

C21H20ClN9O
CAS No.
SMILES

ClC1=CC=C(C=C1)CCNC2=NC=C(C3=NN=C(N4C[C@@]5([H])[C@H](C6=CN=NN6)[C@@]5([H])C4)O3)C=N2
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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Autotaxin-IN-8 Related Classifications

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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.

Keywords:

Autotaxin-IN-83058084-21-9Phosphodiesterase (PDE)p38 MAPKLPL ReceptorERKJNKLysophospholipid ReceptorExtracellular signal regulated kinasesc-Jun N-terminal kinaseA549 cellsp38bleomycin-induced pulmonary fibrosis mouse modelshuman plasmaLPA18:2pulmonary fibrosisERK1/2human normal lung epithelial L132 cellsautotaxinInhibitorinhibitorinhibit

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