2. Neuronal Signaling
  3. Monoamine Oxidase
  4. 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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PXS-4787 Related Antibodies

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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.

PXS-4787 Related Antibodies

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.
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (109.04 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3617 mL 21.8083 mL 43.6167 mL
5 mM 0.8723 mL 4.3617 mL 8.7233 mL
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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3617 mL 21.8083 mL 43.6167 mL 109.0417 mL
5 mM 0.8723 mL 4.3617 mL 8.7233 mL 21.8083 mL
10 mM 0.4362 mL 2.1808 mL 4.3617 mL 10.9042 mL
15 mM 0.2908 mL 1.4539 mL 2.9078 mL 7.2694 mL
20 mM 0.2181 mL 1.0904 mL 2.1808 mL 5.4521 mL
25 mM 0.1745 mL 0.8723 mL 1.7447 mL 4.3617 mL
30 mM 0.1454 mL 0.7269 mL 1.4539 mL 3.6347 mL
40 mM 0.1090 mL 0.5452 mL 1.0904 mL 2.7260 mL
50 mM 0.0872 mL 0.4362 mL 0.8723 mL 2.1808 mL
60 mM 0.0727 mL 0.3635 mL 0.7269 mL 1.8174 mL
80 mM 0.0545 mL 0.2726 mL 0.5452 mL 1.3630 mL
100 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0904 mL
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PXS-4787 Related Classifications

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:

PXS-47872409963-50-2PXS4787PXS 4787Monoamine OxidaseMAOskin treatmentpenetrating skincollagen depositionscar appearancescar tissuemurine models of injury and fibrosisporcine injury modelsInhibitorinhibitorinhibit

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