Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase). Azaserine is a naturally occurring serine derivative diazo compound with antineoplastic properties, Azaserine functions as a purine antagonist and glutamine analogue (glutamine amidotransferase inhibitor) that competitively inhibits pathways in which glutamine is metabolized. Azaserine has been shown to elevate the SOD-2 (manganese-superoxide dismutase (MnSOD)) protein level as well as inhibit the oxidative stress and the expression of VCAM-1 and ICAM-1 in response to TNFα. Research indicates that azaserine has the potential to be used as a probe for identifying the L-(leucine-favoring) system transporter in human T-lymphocytes.
|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||Water ≥ 30 mg/mL|
The hexosamine biosynthesis inhibitor azaserine prevents endothelial inflammation and dysfunction under hyperglycemic condition through antioxidant effects.
Rajapakse AG, et al. Am J Physiol Heart Circ Physiol. 2009 Mar;296(3):H815-22. PMID: 19136606.
LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
TM6008 is a novel PHD inhibitor, which inhibited PHD and stabilized HIF activity in vitro.
ASP9521 is a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
ALW-II-41-27 is a Eph receptor tyrosine kinase inhibitor with an IC50 of 11 nM for EPHA2.
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