Bufalin

Catalog No.S7821 Batch:S782102

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Technical Data

Formula

C24H34O4
Molecular Weight 386.52 CAS No. 465-21-4
Solubility (25°C)* In vitro DMSO 77 mg/mL (199.21 mM)
Ethanol 39 mg/mL (100.9 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[2]
  • Animal Models

    6-7 week old SCID mice injected with MDA-MB-231-LM3.3 cells

  • Dosages

    1.5 mg/kg

  • Administration

    IV

Selleck's Bufalin has been cited by 6 publications

Cell membrane-camouflaged bufalin targets NOD2 and overcomes multidrug resistance in pancreatic cancer [ Drug Resist Updat, 2023, 71:101005] PubMed: 37647746
Bufalin targeting CAMKK2 inhibits the occurrence and development of intrahepatic cholangiocarcinoma through Wnt/β-catenin signal pathway [ J Transl Med, 2023, 21(1):900] PubMed: 38082327
USP24-dependent stabilization of Runx2 recruits a p300/NCOA3 complex to transactivate ADAMTS genes and promote degeneration of intervertebral disc in chronic inflammation mice [ Biol Direct, 2023, 18(1):37] PubMed: 37415159
Alisol B 23-Acetate Increases the Antitumor Effect of Bufalin on Liver Cancer through Inactivating Wnt/β-Catenin Axis [ Comput Math Methods Med, 2022, 2022:6249534] PubMed: 35572840
Elevated Sodium Pump α3 Subunit Expression Promotes Colorectal Liver Metastasis via the p53-PTEN/IGFBP3-AKT-mTOR Axis [ Front Oncol, 2021, 11:743824] PubMed: 34868940
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734] PubMed: 32511305

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.