| Name | R-268712 |
| Description | R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor. |
| In vitro | R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor.?Evaluation of in vitro inhibition indicated that R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). |
| In vivo | Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model.?Additionally, the efficacy of R-268712 in a heminephrectomized anti-Thy1 glomerulonephritis model at doses of 0.3 and 1mg/kg.?R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 250 mg/mL (687.97 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (11.01 mM), Sonication is recommended.
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| Keywords | UUO | Transforming growth factor beta receptors | Transforming growth factor beta | Thy1 nephritis | TGF-β/Smad | TGF-β Receptor | TGF-β | TGFβ | TGF-beta/Smad | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | renal fibrosis | R-268712 | R268712 | R 268712 | Inhibitor | inhibit | HFL-1 | glomerulosclerosis | glomerulonephritis | Cluster of differentiation 246 | CKD | CD246 | Anaplastic lymphoma kinase (ALK) | Anaplastic lymphoma kinase | ALK5 | ALK tyrosine kinase receptor |
| Inhibitors Related | Alectinib | Trimethylamine N-oxide | Melamine | SB-431542 | Hydrochlorothiazide | Crizotinib | Brigatinib | Pirfenidone | A 83-01 | Cetrimonium bromide | Galunisertib | Alantolactone |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | HIF-1 Signaling Pathway Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Bioactive Compounds Library Max | TGF-beta/Smad Compound Library |
United States
