bufalin

Bufalin is a natural product and a Na⁺/K⁺-ATPase inhibitor (IC50 ≈ 40–45 nM) with favorable cell permeability. By binding to α subunits such as ATP1A1, bufalin induces calcium overload and pyroptosis, and can be used for experimental research and therapeutic exploration in various cancers.

Bufalin (compound 2a) is a microbial transformation product of the bufadienolide [1].

Bufalin (Standard) is a reference standard for research and analysis in studies involving Bufalin. Bufalin is an active ingredient and one of the glycosides in the traditional Chinese medicine ChanSu; it is also a bufadienolide toxin originally isolated from the venom of the Chinese toad Bufo gargarizans, with potential cardiotonic and antineoplastic activity. Although the mechanism of action of bufalin is still under investigation, this agent is a specific Na+/K+-ATPase inhibitor and can induce apoptosis in Y cell lines through the activation of the transcription factor AP-1 via a mitogen activated protein kinase (MAPK) pathway.

3-Oxo-bufalin is an active compound isolated from cultured toad liver tissues. It is produced via metabolic pathways as a stereoselectively distinct metabolite of Bufalin, catalyzed by the enzyme 3β-dehydrogenase. Bufalin acts as an inhibitor of Na+/K+-ATPase and possesses antitumor activity.

7β,16α-Dihydroxybufalin, a dihydroxylated derivative of bufalin, demonstrates cytotoxic properties against various cancer cell lines.

19-Hydroxybufalin is a natural product, inhibits epithelial-mesenchymal transition and attenuates the migration and invasion of PC3 cells.

7beta-Hydroxybufalin is a natural product

1beta-Hydroxybufalin is a natural product from animals

MB-Buf is a conjugate of methylene blue and bufalin. Upon photoactivation, MB-Buf selectively degrades GPX4. It induces apoptosis, ferroptosis, and the production of reactive oxygen species (apoptosis). MB-Buf has applications in cancer research, such as in the study of breast cancer.

Antitumor agent-208, an analog of Bufalin, is a potent and orally active antitumor agent. It exhibits antiproliferative activity against tumor cell lines with an IC50 of 0.30-1.09 nM. In MV-4-11 xenograft mouse models, Antitumor agent-208 inhibits tumor growth. It is applicable in cancer research, including studies on acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC).

3-Epicinobufagin (compound IX) serves as a metabolic marker for Bufalin, indicating metabolic status through the detection of its levels in serum and urine.