Sporostatin

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Category Enzyme inhibitors
Catalog number BBF-02940
CAS
Molecular Weight 262.26
Molecular Formula C14H14O5

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Description

It is produced by the strain of Sporormiella sp. M5032. It inhibits cAMP-PDE with ID50 of 41 μg/mL. 1000 μg/mL of Sporostatin has no effect on Gram-positive bacteria, Gram-negative bacteria and Candida albicans.

Specification

Synonyms (+)-Sporostatin
IUPAC Name (4S,6E)-9,11-dihydroxy-4-methyl-4,5-dihydro-1H-3-benzoxecine-2,8-dione
Canonical SMILES CC1CC=CC(=O)C2=C(CC(=O)O1)C=C(C=C2O)O
InChI InChI=1S/C14H14O5/c1-8-3-2-4-11(16)14-9(6-13(18)19-8)5-10(15)7-12(14)17/h2,4-5,7-8,15,17H,3,6H2,1H3/b4-2+/t8-/m0/s1
InChI Key UCKXWYAPJJITRZ-KHVHVRLGSA-N

Properties

Appearance Pale Yellow Crystal
Melting Point 187-200°C
Solubility Soluble in Methanol

Reference Reading

1. Sporostatin, a novel and specific inhibitor of EGF receptor kinase
Y Murakami, A Ishii, S Mizuno, S Yaginuma, Y Uehara Anticancer Res. 1999 Sep-Oct;19(5B):4145-9.
Sporostatin isolated from a fungus of Sporormiella sp.M5032 as an inhibitor of cyclic adenosine 3',5'-monophosphate phosphodiesterase, was found to be a specific inhibitor of epidermal growth factor (EGF) receptor tyrosine kinase in vitro. Its IC50 values were 0.1 microgram/ml (0.38 microM) for EGF receptor kinase, 3 micrograms/ml (11 microM) for ErbB-2, and 100 micrograms/ml (380 microM) or more than that for other kinases including PDGF receptor, v-src and protein kinase C. Kinetic analyses revealed that inhibition of EGF receptor kinase by sporostatin was noncompetitive either with substrate or with ATP. Autophosphorylation of EGF receptor in A431 cells was also inhibited. These results show that sporostatin is a potent and specific inhibitor of EGF receptor kinase.

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