1. Neuronal Signaling
  2. Monoamine Oxidase
  3. PXS-4787

PXS-4787 is a specific and effective pan-LOX (lysyl oxidase) inhibitor for abolishing lysyl oxidase activity. PXS-4787 inhibits LOX with IC50s of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4), respectively.

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PXS-4787 Chemical Structure

PXS-4787 Chemical Structure

CAS No. : 2409963-50-2

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Description

PXS-4787 is a specific and effective pan-LOX (lysyl oxidase) inhibitor for abolishing lysyl oxidase activity. PXS-4787 inhibits LOX with IC50s of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4), respectively[1].

IC50 & Target

2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4)[1]

In Vitro

Lysyl oxidases stabilize the main component of scar tissue, collagen, and drive scar stiffness and appearance[1].
PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species[1].
PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro[1].
PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1[1].

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

Immunofluorescence[1]

Cell Line: Primary human dermal fibroblasts cultured in vitro
Concentration: 0, 1, 10 μM
Incubation Time: 11 days
Result: Significantly reduced in the 10 µM treatment group.

RT-PCR[1]

Cell Line: Cultured fibroblasts and keratinocytes (isolated from five different patients)
Concentration: 10 μM
Incubation Time: 48 hours
Result: Resulted four genes with significant differential expression in fibroblasts and two differentially expressed genes in keratinocytes.
In Vivo

PXS-4787 (3%, oil in water cream; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in murine models of injury and fibrosis under topical application[1].
PXS-4787 (3%, oil in water cream; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].

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

Animal Model: Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1]
Dosage: 3%, oil in water cream; 400 mg cream applied to 16 cm2
Administration: External application; 1, 2 and 3 weeks post-injury; once dailly, for 12 weeks
Result: Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect.
Molecular Weight

229.27

Formula

C10H12FNO2S

CAS No.
SMILES

NC/C=C(CS(=O)(C1=CC=CC=C1)=O)\F

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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PXS-4787 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.

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PXS-4787
Cat. No.:
HY-151498
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