Bufalin

For research use only.

Catalog No.S7821 Synonyms: BF

1 publication

Bufalin Chemical Structure

Molecular Weight(MW): 386.52

Bufalin is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.

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Selleck's Bufalin has been cited by 1 publication

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Biological Activity

Description Bufalin is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.
Targets
SRC-3 [2]
()
SRC-1 [2]
()
Na+/K+-ATPase α3 [1]
(Cell-free assay)
Na+/K+-ATPase α1 [1]
(Cell-free assay)
Na+/K+-ATPase α2 [1]
(Cell-free assay)
40 nM 42.5 nM 45 nM
In vitro

Bufalin strongly promotes SRC-3 protein degradation and binds directly to the coactivator. Bufalin is able to block cancer cell growth at nanomolar concentrations.[2]

In vivo

When incorporated into a nanoparticle delivery system, bufalin is able to reduce tumor growth in a mouse xenograft model of breast cancer. Bufalin sensitizes cancer cells to other targeted chemotherapeutic agents.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: HeLa, MCF-7, A549 cells
  • Concentrations: 2 nM, 5 nM, 7.5 nM
  • Incubation Time: 24 h
  • Method:

    Luciferase assays are performed in HeLa cells transiently transfected with the reporter vector pG5-LUC in combination with expression vectors for pBIND, pBIND SRC-1, SRC-2 or SRC-3 prior to incubation with bufalin of different doses (0, 2, 5 and 7.5 nM) for 24 hours.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: 6-7 week old SCID mice injected with MDA-MB-231-LM3.3 cells
  • Dosages: 1.5 mg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (201.8 mM)
Ethanol 40 mg/mL (103.48 mM)
Water ˂1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 386.52
Formula

C24H34O4

CAS No. 465-21-4
Storage powder
in solvent
Synonyms BF

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID