Home Transmembrane Transporters ATPase inhibitor - Other inhibitor Bufalin For research use only.

Bufalin

Synonyms: BF

Bufalin (BF) 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.

Bufalin Chemical Structure

Bufalin Chemical Structure

CAS: 465-21-4

Selleck's Bufalin has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

Bufalin Related Products

Signaling Pathway

ATPase Signaling Pathways

ATPase Signaling Pathway

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Biological Activity

Description Bufalin (BF) 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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 6-7 week old SCID mice injected with MDA-MB-231-LM3.3 cells
Dosages 1.5 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05942495 Not yet recruiting
Depressive Symptoms|Anxiety Disorders|Persistent|Anxiety Depression
GGZ Noord-Holland-Noord
 November 2023 Not Applicable
NCT05973201 Not yet recruiting
Respiratory Disorder|Lung Infection
Assistance Publique - Hôpitaux de Paris|Ministry of Health France
 September 1 2023 Not Applicable

Chemical Information & Solubility

Molecular Weight 386.52 Formula

C24H34O4
CAS No. 465-21-4 SDF --
Smiles CC12CCC(CC1CCC3C2CCC4(C3(CCC4C5=COC(=O)C=C5)O)C)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (201.8 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 40 mg/mL

Water : ˂1 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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