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.
JNJ-47117096 is potent and selective MELK inhibitor with IC50 of 23 nM.
Phytohemagglutinin is a lectin obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity and involves inflammatory pathways.
Apilimod is a potent IL-12/IL-23 inhibitor, and it is also a cell permeable small molecule which specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay.
10-Hydroxy-trans-2-decenoic acid is the principal lipid component in royal jelly which is the food for queen and larvae honeybees.
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