Description
A xanthonoid with anticancer activity; binds covalently to SPTSSB (Ki = 1.5 µM; kinact = 0.05 min-1) and inhibits de novo sphingolipid biosynthesis; activates caspases in T47D breast cancer cells (EC50 = 0.78 µM); inhibits binding of anti-apoptotic proteins to a BH3 peptide (IC50s = 1.47, 1.21, 2.02, 0.66, 1.06, and 0.79 μM for Bcl-xL, Bcl-2, Bcl-W, Bcl-B, Bfl-1, Mcl-1, respectively); binds to the transferrin receptor (IC50 = 4.1 µM); reduces growth of a variety of cancer cell lines (GI50s = 0.115-1 µM) and induces apoptosis in T47D cells; a slow inhibitor of inward-rectifying potassium channel 2.1 (Kir2.1; IC50 = <0.1 µM)
Formal name: 2-methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-buten-1-yl)-11-(4-methyl-3-penten-1-yl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-2Z-butenoic acid
Synonyms: GA|β-Guttiferin
Molecular weight: 628.8
CAS: 2752-65-0
Purity: ≥95% (mixture of epimers)
Formulation: A crystalline solid
Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Activators|Caspases||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Lipid Biochemistry|Sphingolipids
