Gambogenic acid

Research use only, not for human use.

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge.

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells; specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=8.6 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination; synergistically potentiates bortezomib-induced apoptosis in multiple myeloma; also induces proteasomal degradation of CIP2A and sensitizes hepatocellular carcinoma to anticancer agents.

Western Blot Analysis Cell Line:SCLC cell lines (NCI-H446/NCI-H1688) Concentration:1.1-1.3 μM for NCI-H446 cells, 2-2.3 μM for NCI-H1688 cells Incubation Time:24 h Result:Increased the expression of cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins.

Animal Model:SCLC mouse xenograft modelDosage:4-12 mg/kg Administration:i.v., every 2 days, 14 days Result:Increased the expression of pro-apoptotic proteins (cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins).Decreased the anti-apoptotic proteins (Bcl-2).

GNA

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

173932-75-7

630.778

C38H46O8

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (158.54 mM)

O=C(O)/C(C)=C\C[C@]([C@@]12OC3=C4C(O)=C(C/C=C(C)/CC/C=C(C)\C)C(O)=C3C/C=C(C)\C)(OC(C)(C)[C@]2([H])C5)C([C@]5([H])C=C1C4=O)=O

(Z)-4-((1S,3aR,5S,12aS)-9-((E)-3,7-dimethylocta-2,6-dien-1-yl)-8,10-dihydroxy-2,2-dimethyl-11-(3-methylbut-2-en-1-yl)-4,7-dioxo-1,2,5,7-tetrahydro-1,5-methanofuro[2,3-d]xanthen-3a(4H)-yl)-2-methylbut-2-enoic acid

(-20℃)

With Ice Pack

≥ 2 years