loxl2

PAT-1251 is an inhibitor of LOXL2 with IC50s of 10, 0.12, and 0.16 μM for the mouse, rat, and dog and can be used in studies about fibrotic diseases.

Lenumlostat is an orally available, selective and potent lysyl oxidase-like protein 2 (LOXL2) inhibitor with inhibitory effects on hLOXL2, hLOXL3 and LOXL2 for the study of fibrotic diseases.

(2-Chloropyridin-4-yl)methanamine hydrochloride is a selective LOXL2 inhibitor with an IC50 of 126 nM.

PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.

PXS-5153A is an effective, selective, and fast-acting inhibitor of lysyl oxidase like 2/3 enzymes with enzymatic activity almost entirely blocked within 15 minutes. PXS-5153A could reduce crosslinks and ameliorates fibrosis.

LOX-IN-3 dihydrochloride, an inhibitor of lysyl oxidase (LOX), inhibits bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM) activities.

Simtuzumab is a monoclonal antibody against lysyl oxidase-like protein 2 (LOXL2). Simtuzumab can be used to treat primary sclerosing cholangitis (PSC) and is not effective in patients with bridging fibrosis or compensatory cirrhosis caused by non-alcoholic steatohepatitis.

LOXL2/sGC modulator-1 (Compound 11k) is an LOXL2 inhibitor with an IC₅₀ of 0.13 μM and acts as an sGC activator. It shows good selectivity for LOX (IC₅₀ > 45.9 μM) and LOXL3 (IC₅₀ = 1.30 μM). In the presence of the gGC inhibitor ODQ, it significantly increases intracellular cGMP levels. LOXL2/sGC modulator-1 effectively inhibits hypoxia-induced collagen deposition and cross-linking while promoting vasodilation. This compound is useful for researching pulmonary arterial hypertension.

LOXL2/sGC modulator-2 (Compound 9k) is a selective, orally active dual-target modulator of lysyl oxidase-like protein 2 (LOXL2) and soluble guanylate cyclase (sGC). It inhibits LOXL2 with an IC50 of 0.1 μM and acts as an sGC activator. This compound can improve vascular remodeling and reduce pulmonary arterial pressure while downregulating PKG1, PCNA, α-SMA, collagen I, and fibronectin levels. LOXL2/sGC modulator-2 is useful for studying pulmonary arterial hypertension.

LOX-IN-5 tosylate (compound 22) is a selective oral inhibitor of lysyl oxidase-like 2 (LOXL2) with an IC50 of less than 300 nM, and it exhibits anti-fibrotic properties.

PAT-1251 Hydrochloride is a potent, selective, and oral inhibitor of lysyl oxidase-like 2 (LOXL2), targeting hLOXL2 and hLOXL3 with IC50 values of 0.71 and 1.17 μM, respectively.

PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis

PXS-4787 hydrochloride is a specific and potent pan-lysyl oxidase inhibitor that effectively eliminates the activity of lysyl oxidase. It exhibits varying IC50 values against different forms of the enzyme, including 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4). In addition, PXS-4787 hydrochloride reduces the deposition and cross-linking of collagen I secreted by human fibroblasts.

Escin IA (Escin IA;Aescin IA) is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].

PXS-4787 is a potent and selective inhibitor of lysyl oxidase (LOX) with broad-spectrum activity. It effectively suppresses lysyl oxidase activity by acting on its mechanisms. The compound displays inhibitory effects with IC50 values of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4), respectively [1].

PXS-6302 is an irreversible inhibitor of lysyl oxidase with IC50s of 3.7 μM for Bovine LOX, 3.4 μM for rh LOXL1, 0.4 μM for rh LOXL2, 1.5 μM for rh LOXL3, 0.3 μM for rh LOXL4, respectively. PXS-6302 can readily penetrate the skin, reduces collagen deposition and cross-linking, and significantly improves scar appearance without reducing tissue strength. PXS-6302 also has potentially broader applications in other fibrotic diseases.

PXS-6302 hydrochloride is a potent irreversible lysine oxidase (LOX) inhibitor, inhibiting Bovine LOX, rh LOXL1, rh LOXL2, rh LOXL3, and rh LOXL4 with IC50 of 3.7 μM, 3.4 μM, 0.4 μM, 1.5 μM, and 0.3 μM, respectively. PXS-6302 hydrochloride penetrates easily through the skin and is able to reduce collagen accumulation, significantly improving the appearance of scars.

Escin IA (Standard) is a reference standard for research and analysis in studies involving Escin IA. Escin IA (Escin IA;Aescin IA) is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].