GNA002

Research use only, not for human use.

GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain.

GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination; GNA002 is a relatively more potent EZH2 interacting agent than GNA, significantly suppresses H3K27Me3 and effectively reactivated PRC2-silenced tumor suppressor genes.

Cell Proliferation Assay Cell Line:Numerous cancer cell lines Concentration:10 μM Incubation Time:72 hours Result:Inhibited the proliferation of numerous cancer cell lines with IC50s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11.Apoptosis Analysis Cell Line:HN-4 and Cal-27 head and neck cancer cells Concentration:2 μM Incubation Time:24 hours Result:Induced cellular apoptosis in human cancer cells.Western Blot Analysis Cell Line:Cal-27 head and neck cancer cells Concentration:0.1, 0.2, 0.5, 1, 2, 4 μM Incubation Time:48 hours Result:Reduced H3K27Me3 levels.

Animal Model:Male BALB/C Nude mice aged 30-35 days and weighing 18-22 g, bearing Cal-27 xenograft tumors Dosage:100 mg/kg Administration:Oral administration; daily Result:Decreased the size and weight of tumors formed by Cal-27 cells.

GNA-002

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

1385035-79-9

701.901

C42H55NO8

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (35.62 mM)

CCOCCNC(=O)C(=CCC12C(=O)C3CC(C14C(=C3)C(=O)C5=C(C(=C(C(=C5O4)CC=C(C)C)O)CC=C(C)CCC=C(C)C)O)C(O2)(C)C)C

(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)-N-(2-ethoxyethyl)-2-methylbut-2-enamide

(-20℃)

With Ice Pack

≥ 2 years