KS 504a
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| Category | Enzyme inhibitors |
| Catalog number | BBF-03607 |
| CAS | 122022-77-9 |
| Molecular Weight | 367.27 |
| Molecular Formula | C7H3Cl7O2 |
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Description
It is produced by the strain of Mollisia ventosa KAC-1148. KS 504a inhibited Ca2+ and calmodulin dependent cyclic-nucleotide phosphodiesterase with an IC50 of 122 μmol/L.
Specification
| Synonyms | KS-504a; KS-504b; BRN 4354490; 1-Oxaspiro(2.4)heptan-5-ol, 2,4,4,6,6-pentachloro-7-(dichloromethylene)- |
| IUPAC Name | 2,4,4,6,6-pentachloro-7-(dichloromethylidene)-1-oxaspiro[2.4]heptan-5-ol |
| Canonical SMILES | C1(C(C(=C(Cl)Cl)C2(C1(Cl)Cl)C(O2)Cl)(Cl)Cl)O |
| InChI | InChI=1S/C7H3Cl7O2/c8-2(9)1-5(4(10)16-5)7(13,14)3(15)6(1,11)12/h3-4,15H |
| InChI Key | PHUXLMFYGOIQKL-UHFFFAOYSA-N |
Properties
| Appearance | Colorless Flake Crystal |
| Boiling Point | 485°C at 760 mmHg |
| Melting Point | 102-102.5°C |
| Density | 1.96 g/cm3 |
Reference Reading
1. Calmodulin antagonistic action of KS-504a, a novel metabolite of the fungus Mollisia ventosa
S Nakanishi, K Kuroda, K Osawa, H Kase Agric Biol Chem. 1990 Oct;54(10):2697-702.
KS-504a inhibited bovine brain calmodulin-dependent cyclic nucleotide phosphodiesterase (CaM-PDE) with an IC50 value of 122 microM. The inhibition was reversed by a high concentration of calmodulin. Calmodulin-independent activities of the enzyme were not affected by the compound at the same concentration ranges. Ca2(+)-dependent interaction of the compounds with calmodulin was shown using hydrophobic fluorescence probes. These data indicated that the compound exerted its effects on CaM-PDE by interacting with calmodulin. KS-504a also inhibited other calmodulin-dependent enzymes at different concentration ranges; myosin light chain kinase was inhibited at the lowest concentrations with an IC50 value of 6.3 microM. The inhibition mechanism was competitive with respect to calmodulin and non-competitive to ATP.
2. KS-504 compounds, novel inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase from Mollisia ventosa
S Nakanishi, K Ando, I Kawamoto, T Yasuzawa, H Sano, H Kase J Antibiot (Tokyo). 1989 Dec;42(12):1775-83. doi: 10.7164/antibiotics.42.1775.
Novel inhibitors of Ca2+ and calmodulin-dependent cyclic nucleotide phosphodiesterase were isolated from the culture broth of a fungus, Mollisia ventosa KAC-1148. They were designated as KS-504a, KS-504b and KS-504d. A degradative product of KS-504a, called KS-504e, was also isolated and found to inhibit the enzyme. The 50% inhibitory concentration (IC50) values of KS-504a, KS-504b, KS-504d and KS-504e for bovine brain enzyme were 122, 109, greater than 500 and 139 microM, respectively.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
