Adjudin (also known as AF-2364) is a potent Cl- channel blocker, with a superior mitochondria-inhibitory effect. Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinoma cell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC50 of Adjudin is determined to be 58.0 µM, 13.8 µM, 72.3 µM and 52.7 µM against SGC-7901, MDA-MB-231, Smmc-7721 and MIA Paca-2 cells, respectively, after treatment for 24 h. Similar results are obtained in other human and mice cancer cell lines. The IC50 of Adjudin in A549 cells and PC3 cells is 63.1 µM and 93.0 µM, respectively. Adjudin-treated mice show significant tumor growth inhibition compared with the control group (P<0.0001 in the human lung carcinoma cells A549 and P=0.006 in the prostate carcinoma cells PC3).
|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: ≥ 30 mg/mL|
Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans.
Li K, et al. Hum Reprod. 2013 Jan;28(1):47-59. PMID: 23117128.
AZ-33 is a potent lactate dehydrogenase A (LDHA) inhibitor with IC50 of 0.5 μM.
2-Aminoadipic acid is a six-carbon homolog of glutamate and a gliotoxic compound. It is generally used to considerably reduce the number of astroglia in cerebellar cultures that acts as a model to study the mechanisms of a-aminoadipic acid induced glial toxicity.
1-Naphthyl isothiocyanate (NITC) can be used as a source of thiourea moiety to synthesize derivatives of calixarenes to be used as anion acceptors.
LOC14 is a potent PDI (protein disulfide isomerase) inhibitor with EC50 value of 500 nM.
Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant.
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