General descriptionA cardiotonic steroid isolated from Bufo species toads that potently inhibits ouabain-sensitive Na+,K+-ATPase activity. Induces apoptosis in various human cell lines such as leukemia HL60 and U937 cells by altering the expression of apoptosis-related genes. Reported to stimulate the activities of p21 activated kinase (PAK) and c-Jun Kinase (JNK) in leukemic cell lines. Induces a transient increase in the expression of Tiam1 mRNA in U937 cell lines (~100 nM). Bufalin also down-regulates gene expression of the intracellular signaling protein 14-3-3 in rat lens, probably a consequence of Na+-K+-ATPase inhibitors. Reduces the level of topoisomerase II in human leukemia cells.A cardiotonic steroid isolated from toads of Bufo species that potently inhibits ouabain-sensitive Na+,K+-ATPase activity (IC50 = 1.4 nM). Induces apoptosis in various human cell lines such as leukemia HL-60 and U937 cells by altering the expression of apoptosis-related genes. Reported to stimulate the activities of p21 activated kinase (PAK) and c-Jun Kinase (JNK) in leukemic cell lines. Induces a transient increase in the expression of Tiam1 mRNA in U937 cell lines (~100 nM). Bufalin also down-regulates gene expression of the intracellular signaling protein 14-3-3 in rat lens, probably a consequence of Na+,K+-ATPase inhibition. Reduces the level of topoisomerase II in human leukemia cells.Biochem/physiol ActionsCell permeable: noPrimary TargetOuabain-sensitive Na+,K+-ATPase activityProduct does not compete with ATP.Reversible: noTarget IC50: 1.4 nM against ouabain-sensitive Na+,K+-ATPase activityPackagingPackaged under inert gasWarningToxicity: Highly Toxic (H)ReconstitutionFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.Other NotesDue to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.Kurosawa, M., et al. 2000. Am. J. Physiol.278, C500.Kawazoe, N., et al. 1999. Oncogene 18, 2413.McGowan, M.H., et al. 1999. J. Pharmacol. Exp. Ther. 289, 1559.Watabe, M., et al. 1998. Oncogene 16, 779.Hashimoto, S., et al. 1997. Leuk. Res. 21, 875.Morris, J.F., et al. 1997. Comp. Biochem. Physiol. A Physiol. 118, 599.Brownlee, A.A., et al. 1990. Clin. Sci.78, 169.Legal InformationCALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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