| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
Soluble in water (up to 1 mg/ml) or in DMSO | [form ]
solid | [color ]
Off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in distilled water or DMSO may be stored at -20°C for up to 1 month. |
| Hazard Information | Back Directory | [Description]
Koningic acid (KA; 74310-84-2) is a potent and selective inhibitor of glyceraldehyde-3-phosphate dehydrogenase (GAPDH).1? Inhibition is irreversible and proceeds via nucleophilic attack of an active site cysteine on the epoxide moiety2, Ki = 1.1 μM for rabbit muscle GAPDH3. KA can selectively kill high-glycolytic cancer cells via glucose dependent ATP depletion.4 Has been used in a predictive model for selective targeting of the Warburg effect, the most prominent hallmark of cancer cell metabolism.5 | [Uses]
Heptelidic acid is an inhibitor of GAPDH and certain DNA polymerases. | [References]
1) Endo et al. (1985), Specific inhibition of glyceraldehyde-3-phosphate dehydrogenase by koningic acid (heptelidic acid); J. Antibiot., 38 920
2) Sakai et al. (1991), Identification of koningic acid (heptelidic acid)-modified site in rabbit muscle glyceraldehyde-3-phosphate dehydrogenase; Biochim. Biophys. Acta, 1077 192
3) Sakai et al. (1988), Inactivation of rabbit muscle glyceraldehyde-3-phosphate dehydrogenase by koningic acid; Biochim. Biophys. Acta, 952 297
4) Kumagai et al. (2008), Glucose-dependent active ATP depletion by koningic acid kills high-glycolytic cells; Biochem. Biophys. Res. Commun. 365 362
5) Liberti et al. (2017), A Predictive Model for Selective Targeting of the Warburg Effect through GAPDH Inhibition with a Natural Product; Cell Metab., 26 648 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Creative Enzymes
|
| Tel: |
1-516-855-7709 |
| Website: |
www.creative-enzymes.com |
|