SW033291 inhibition of 15-PGDH was noncompetitive versus PGE2 over concentrations up to 40 μM PGE2. SW033291 also demonstrated selective high-affinity interaction with 15-PGDH in thermal denaturation assays. Treatment of A549 cells with SW033291 increased PGE2 levels by 3.5-fold at 500 nM, with 50% of maximal stimulation (EC50) at ~75 nM.
|Source||Sci Rep (2018). Figure 5. SW033291|
|Method||Treatment of diseased tendon stromal cells with inhibitors of 15-PGDH|
|Cell Lines||tendon stromal cells|
|Incubation Time||2 h|
|Results||In incubations of IL-1β stimulated diseased tendon stromal cells with either indomethacin or SW033291, we found significantly lower concentrations of 15-oxo-LXA4 and 14-oxo-MaR1 levels, and a corresponding increase in the levels of 15-epi-LXA4 and MaR1|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration.
Zhang Y,et.al. Science. 2015 Jun 12;348(6240). PMID: 26068857.
|Related Dehydrogenase Products|
DS-1001b is a potent mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor with antitumor activity.
Ivosidenib is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
BAY1436032 specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells.
Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.