Bohemine served as a kinase inhibitor in the activation of bovine oocytes. Inhibition of DNA synthesis in oocytes was shown to be reversible, because after removal from boheminesupplemented medium the activated oocytes started to synthesize DNA. An attempt at elucidating the molecular basis of bohemine activity was undertaken through employing proteomics technology.
|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|
Diverse effects of the cyclin-dependent kinase inhibitor bohemine: Concentration- and time-dependent suppression or stimulation of hybridoma culture
Franek F, et al. Cytotechnology. 2001 Jul;36(1-3): 117–123. PMID: 19003322.
In vivo metabolism of 2,6,9-trisubstituted purine-derived cyclin-dependent kinase inhibitor bohemine in mice: glucosidation as the principal metabolic route.
Chmela Z, et al. Drug Metab Dispos. 2001 Mar;29(3):326-34. PMID: 11181503.
LY2334737 is an orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity.
TUG-891 is a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120).
GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).
EXP-3174 is a potent AT1 antagonist with Kis of 0.57 and 0.67 nM for rat and human forms, respectively.
NAV-2729 is a selective ARF6 inhibitor with IC50 value of 1.0 μM.
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