AI-1 is a negative regulator of Nrf2. AI-1 promotes Nrf2 activation via the covalent modification of Kelch-like ECH-associated protein 1 (Keap1). Biochemical studies indicate that an aromatic chloride present within the AI-1 molecule undergoes a nucleophilic aromatic substitution reaction with cysteine thiols of Keap1.
|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||DMSO: ≥15 mg/mL|
Involvement of luxS in Biofilm Formation by Capnocytophaga ochracea.
Hosohama-Saito K, et al. PLoS One. 2016 Jan 22;11(1):e0147114. PMID: 26800339.
Genome-wide RNA sequencing analysis of quorum sensing-controlled regulons in the plant-associated Burkholderia glumae PG1 strain.
Gao R, et al. Appl Environ Microbiol. 2015 Dec;81(23):7993-8007. PMID: 26362987.
ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.
ML-265 (TEPP-46) is a potent and selective activator of recombinant pyruvate kinase M2 (PKM2).
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.
Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase).
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