| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C10H12FNO2S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
PXS-4787 is a specific, effective pan-LOX (lysyl oxidase) inhibitor that abolishes lysyl oxidase activity, with IC50 values of 2 μM against bovine LOX, 3.2 μM against recombinant human LOXL1, 0.6 μM against recombinant human LOXL2, 1.4 μM against recombinant human LOXL3, and 0.2 μM against recombinant human LOXL4[1]. Its molecular formula is C10H12FNO2S, with a molecular weight of 229.27 g/mol.
Physical & Chemical Properties
| CAS Number | 2409963-50-2 |
|---|---|
| Molecular Formula | C10H12FNO2S |
| Molecular Weight | 229.27 g/mol |
| SMILES | NC/C=C(CS(=O)(C1=CC=CC=C1)=O)\F |
| Signaling Pathway | Neuronal Signaling |
| Solubility | In Vitro: DMSO: 25 mg/mL (109.04 mM; Requires sonication and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & 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]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (109.04 mM) | requires sonication and warming; use freshly opened DMSO (absorbed moisture lowers solubility) |
Data provided by the manufacturer.
In Vitro
Lysyl oxidases stabilize collagen, the main component of scar tissue, and determine scar stiffness and appearance[1]. At 0-10 μM for 15 min-4 h, PXS-4787 inhibits lysyl oxidase in a dose- and time-dependent manner and shows comparable inhibitory activity across species[1]. Primary human dermal fibroblasts tolerate PXS-4787 well at 0-100 μM for 72 h, and at 10 μM for 11 d it reduces collagen formation, deposition and crosslinking in these cells cultured in vitro[1]. In fibroblasts and keratinocytes, PXS-4787 (10 μM; 48 h) induces differential gene expression, including COL1A1, LOX, GAPDH and PGK1[1].
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
Topical PXS-4787 (3% oil in water cream; applied externally once daily for 28 days) reduces collagen deposition and cross-linking in murine models of injury and fibrosis[1]. Topical PXS-4787 (3% oil in water cream; applied externally once daily for 12 weeks) also significantly improves scar appearance in porcine injury models, without reducing tissue strength[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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