Napabucasin

Napabucasin
Clinical data
Drug class	STAT3 inhibitor
Identifiers
	IUPAC name 2-acetylbenzo[f][1]benzofuran-4,9-dione;
CAS Number	83280-65-3;
PubChem CID	10331844;
Chemical and physical data
Formula	C14H8O4
Molar mass	240.214 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O;
	InChI InChI=1S/C14H8O4/c1-7(15)11-6-10-12(16)8-4-2-3-5-9(8)13(17)14(10)18-11/h2-6H,1H3; Key:DPHUWDIXHNQOSY-UHFFFAOYSA-N;

Napabucasin (BBI-608) is a natural product found in the inner bark of the tree Handroanthus impetiginosus, that acts as an inhibitor of the transcription factor protein STAT3. It has potential applications in the treatment of cancer, acting as a stemness inhibitor.^[1]^[2]^[3]^[4]^[5]

References

^ Löcken H, Clamor C, Müller K (July 2018). "Napabucasin and Related Heterocycle-Fused Naphthoquinones as STAT3 Inhibitors with Antiproliferative Activity against Cancer Cells". Journal of Natural Products. 81 (7): 1636–1644. Bibcode:2018JNAtP..81.1636L. doi:10.1021/acs.jnatprod.8b00247. PMID 30003778.
^ Lee C, Cheung ST (October 2019). "STAT3: An Emerging Therapeutic Target for Hepatocellular Carcinoma". Cancers. 11 (11): 1646. doi:10.3390/cancers11111646. PMC 6895841. PMID 31731457.
^ Ahmadi ES, Tajbakhsh A, Iranshahy M, Asili J, Kretschmer N, Shakeri A, et al. (2020). "Naphthoquinone Derivatives Isolated from Plants: Recent Advances in Biological Activity". Mini Reviews in Medicinal Chemistry. 20 (19): 2019–2035. doi:10.2174/1389557520666200818212020. PMID 32811411.
^ Shao Z, Wang H, Ren H, Sun Y, Chen X (July 2023). "The Anticancer Effect of Napabucasin (BBI608), a Natural Naphthoquinone". Molecules. 28 (15): 5678. doi:10.3390/molecules28155678. PMC 10420168. PMID 37570646.
^ Yang X, Ma G (January 2026). "Recent progress of napabucasin as privileged scaffold in the discovery of anticancer agents". European Journal of Medicinal Chemistry. 305 118559. doi:10.1016/j.ejmech.2026.118559. PMID 41494471.