General description
A cell-permeable anacardic acid (Cat. No. 172050) analog that inhibits protein SUMO (Cat. No. 662037, 662039, and 662042) modification (IC50 = 3.0 µM using RanGAP1-C2 as substrate) in an ATP-dependent manner by selectively targeting SUMO-activating enzyme E1 (Cat. No. 662073 and 662074) and interfering with E1-SUMO intermediate formation independent of E1 active site cysteine. Both ginkgolic acid and anacardic acid are shown to effectively decrease overall SUMOylation of 293T cellular proteins, including p53, in a dose-dependent manner, while neither compound is effective in affecting overall cellular protein ubiquitination or histone H4K8 acetylation in 293T cultures, although both compounds are shown to inhibit histone lysine acetylation by PCAF (Cat. No. 124026) in cell-free acetylase assays.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
SUMO-activating enzyme E1
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Physical form
A 25 mM (2 mg/231 µl) sterile-filtered solution of Ginkgolic Acid (15:1) (Cat. No. 345887) in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. Use only fresh DMSO for further dilutions.
Other Notes
Fukuda, I., et al. 2009. Chem. Biol.16, 133.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51461517
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5081970001