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 immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.

Bufalin Chemical Structure

Bufalin Chemical Structure

CAS No. 465-21-4

Purity & Quality Control

Bufalin Related Products

Signaling Pathway

ATPase Signaling Pathways

ATPase Signaling Pathway

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 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
NCT06360809 Recruiting
Breast Cancer
Institut Nacional d''Educacio Fisica de Catalunya|ICFO - The Institute of Photonics Sciences|Hospital Clinic of Barcelona|Institut d''Investigacions Biomèdiques August Pi i Sunyer|Universidad San Jorge
 March 22 2024 Not Applicable
NCT06240078 Recruiting
Pulmonary Disease Chronic Obstructive|Sexual Health|Loneliness|Well-Being Psychological
Vejle Hospital|Region of Southern Denmark
 February 20 2024 --

Chemical Information & Solubility

Molecular Weight 386.52 Formula

C24H34O4
CAS No. 465-21-4 SDF --
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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