Bruceantinol 

Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC₅₀ = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells^[1][2][3].

IC₅₀: 2.4 pM (STAT3 DNA-binding ability)^[2]

Bruceantinol (Compound 4) (5-40 μM) shows strong inactivation effect against PepMoV with a minimum inhibitory concentration of 10 μM in C. annuum^[1].
Bruceantinol (Compound BOL) (0-100 nM, 24 h) significantly decreases colony formation in a dose-dependent manner across the human CRC cell line panel (HCT116, HCT116 p53^-/-, HCA-7, H630 and H630R1)^[2].
Bruceantinol (300 nM, 24 h) alters the expression of 25 proteins (p-STAT3, MCL-1, c-Myc, and cleaved caspase-7) in HCT116 cells, in which the STAT3-mediated signal pathway is significantly suppressed^[2].
Bruceantinol (30 nM, 0-24 h) inhibits STAT3 phosphorylation in HCT116 cells^[2].
Bruceantinol (10-300 nM, 24 h) potently suppresses IL-6-induced activation of STAT3 in CRC cells^[2].
Bruceantinol (0-1000 nM, 24 h) significantly decreases expression of MCL-1, c-Myc, and surviving in a dose-dependent manner^[2].
Bruceantinol (0-1600 nM, 24-48 h) reduces breast cancer cell (MCF-7 and MDA-MB-231) growth^[3].
Bruceantinol (100-400 nM, 24 h) results in a gradual decrease in the number of cells in G0/G1 with a corresponding increase in the cell numbers in S and G2/M in MCF-7 and MDA-MB-231 cells^[3].
Bruceantinol (100-400 nM, 10 h) decreases CDK2/4/6 protein levels dependently on the proteasome pathway in MCF-7 and MDA-MB-231 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bruceantinol (Compound BOL) (2-4 mg/kg, i.p., thrice per week) inhibits p-STAT3 expression in mice bearing HCT 116 xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

606.61

C₃₀H₃₈O₁₃

53729-52-5

Solid

White to light yellow

COC([C@]12[C@@]3([H])[C@@]4(CO2)[C@@]([C@H]([C@@H]1O)O)([H])[C@@]5([C@@](C(C)=C(C(C5)=O)O)([H])C[C@@]4([H])OC([C@@H]3OC(/C=C(C)/C(C)(C)OC(C)=O)=O)=O)C)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Seung Mok Ryu, et al. Quassinoids isolated from Brucea javanica inhibit pepper mottle virus in pepper. Virus Res. 2017 Jan 2;227:49-56.  [Content Brief]

  [2]. Ning Wei, et al. Targeting colon cancer with the novel STAT3 inhibitor bruceantinol. Oncogene. 2019 Mar;38(10):1676-1687.  [Content Brief]

  [3]. Sun, L., et al., (2024). Bruceantinol works as a CDK2/4/6 inhibitor to inhibit the growth of breast cancer cells. Chemico-biological interactions, 395, 110999.  [Content Brief]