2. Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt
  3. Phosphodiesterase (PDE) ERK JNK p38 MAPK
  4. ATX inhibitor 26

ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with anIC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model.

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ATX inhibitor 26 Chemical Structure

ATX inhibitor 26 Chemical Structure

CAS No. : 2940248-11-1

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ATX inhibitor 26 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Description

ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with anIC50 of 57 nM in human plasma. ATX inhibitor 26 inhibits cell migration and collagen gel contraction. ATX inhibitor 26 has significant anti-fibrotic effects, reducing collagen deposition in a Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis model[1].

IC50 & Target[1]

Autotaxin

57 nM (IC50)

In Vitro

ATX inhibitor 26 (Compound 27a) (500 nM) has an excellent inhibitory activity against ATX (94.1% inhibition, IC50: 39.2 nM) and Lysophospholipase D (LysoPLD) (over 90% inhibition, IC50: 57.2 nM) in human plasma[1].
ATX inhibitor 26 (3.0 μM, 12-48 h) significantly suppresses LPC/TGF-β-induced MAPK activation in L132 cells, A549 cells and WI38 cells[1].
ATX inhibitor 26 (0-6.0 μM, 0.5-6.0 h) dose- and time-dependently regulates the MAPK signaling, reducing the phosphorylation levels of ERK, p38, and JNK at doses ≥0.5 μM within 30 min in L132 cells[1].
ATX inhibitor 26 (3.0 μM, 0-48 h) significantly reduces both basal and TGF-β-induced migration of A549 cells and collagen gel contraction of WI38 cells[1].

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

ATX inhibitor 26 Related Antibodies

Western Blot Analysis[1]

Cell Line: L132 cells
Concentration: 0.1, 0.5, 1.0, 3.0, 6.0 μM
Incubation Time: 0.5, 1.0, 3.0, 6.0 h
Result: Dose- and time-dependently reduced the phosphorylation levels of ERK, p38, and JNK, with effects observed at dose as low as 0.5 μM and within 30 min of treatment.
Significantly suppressed LPC (1 μM) and TGF-β (5 ng/ml)-induced MAPK pathway activation.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 3.0 μM
Incubation Time: 48 h
Result: Significantly reduced both basal and TGF-β-induced migration of epithelial cells.
Parmacokinetics
Species Dose SampleTime Route Indicator value
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Tmax 0.5 hr
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. Cmax 1093.2 μg/mL
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. T1/2 7.5 hr
Mice 30 mg/kg 0.5, 1, 2, 4, 8, 24 h o.a. AUClast 3088.3 ng·h/mL
In Vivo

ATX inhibitor 26 (Compound 27a) (1 or 2 mg/kg, p.o., once a day for 21 days) reduces collagen deposition, LPAR1, and p-ERK1/2 expression, while decreasing mRNA levels of α-SMA, Col1A1, and pro-inflammatory markers IL-6, IL-1β, and INF-γ in a BLM-induced pulmonary fibrosis model[1].

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

Animal Model: male C57BL/6 mice (8 weeks old) were given BLM (1.8 U/kg/mouse) through intratracheal injection to induce pulmonary fibrosis[1].
Dosage: 1 or 2 mg/kg
Administration: oral gavage (p.o.), once a day for 21 days (7 days prior to BLM administration and 14 days post-BLM), and then collects lung tissue.
Result: Increased survival of BLM-induced pulmonary fibrosis mice.
Significantly reduced collagen deposition, LPAR1, and p-ERK1/2 expression in pulmonary tissue.
Significantly decreased mRNA levels of α-SMA, Col1A1, and pro-inflammatory markers IL-6, IL-1β, and INF-γ in a BLM-induced pulmonary fibrosis model.
Did not induced significant histopathological abnormalities in the liver, kidney, and spleen and notable changes in serum biochemical marker.
Molecular Weight

452.29

Formula

C18H19Cl2N7O3
CAS No.
SMILES

ClC1=CC(Cl)=CC(COC(N2CCC(C3=NN=C(NCC4=CN=NN4)O3)CC2)=O)=C1
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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ATX inhibitor 26 Related Classifications

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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.

Keywords:

ATX inhibitor 262940248-11-1ATX inhibitor26ATX inhibitor-26Phosphodiesterase (PDE)ERKJNKp38 MAPKExtracellular signal regulated kinasesc-Jun N-terminal kinaseAutotoxinInhibitorBleomycin (BLM)MAPKFibrosisinhibitorinhibit

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