Drug intelligence / Profile preview

jolkinolide b

Development stage
Preclinical
Modality
Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Unknown (preclinical Studies Use Cell Culture And Animal Models)
01

Overview

**Jolkinolide B** is a natural ent-abietane-type diterpenoid lactone isolated primarily from Euphorbia fischeriana and other Euphorbia species[1][2][3][4][6][8]. It exhibits broad pharmacological activity, including anticancer, anti-inflammatory, anti-tuberculosis, and antiviral effects. Mechanistically, Jolkinolide B induces apoptosis in various cancer cells (including gastric cancer, lung cancer, breast cancer, hepatocellular carcinoma, lymphoma, and leukemia)[1][4][6][8]; triggers cell cycle arrest via the ATR-CHK1-CDC25A-Cdk2 pathway[4]; inactivates the β-catenin signaling pathway and downregulates migration/invasion markers in hepatocellular carcinoma[6]; suppresses JAK2/STAT3 signaling in rheumatoid arthritis, leading to decreased inflammation and bone destruction[3]. It also downregulates Akt, STAT3, and mTOR protein levels in endothelial cells[8].

Other names
37905-08-1(1S,3R,8R,10R,11R,12R,17R)-5,12,16,16-tetramethyl-2,7,9-trioxahexacyclo[9.8.0.01,3.04,8.08,10.012,17]nonadec-4-en-6-oneBisoxireno(1,10a:3,4)phenanthro(3,2-b)furan-9(7aH)-one
02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)CDC25A (Cell division cycle 25A phosphatase)CDK2 (Cyclin-dependent kinase 2)JAK2 (Janus kinase 2)MSI2 (Musashi RNA-binding protein 2)STAT3 (Signal Transducer and Activator of Transcription 3)mTOR (Mammalian target of rapamycin kinase)CTNNB1 (Beta-catenin)

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