WF14865A

WF14865A

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Category Enzyme inhibitors
Catalog number BBF-01632
CAS
Molecular Weight 367.4
Molecular Formula C16H25N5O5

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Description

WF14865A is a cathepsins B and L inhibitor with IC50 of 8.4 X 10(-9) and 6.6 X 10(-8) mol/L, respectively. It is produced by Aphanoascus fulvescens.

Specification

Synonyms WF-14865A

Properties

Appearance Colorless Powder

Reference Reading

1. WF14865A and B, new cathepsins B and L inhibitors produced by Aphanoascus fulvescens. I. Taxonomy, production, purification and biological properties
T Otsuka, Y Muramatsu, T Nakanishi, H Hatanaka, M Okamoto, M Hino, S Hashimoto J Antibiot (Tokyo). 2000 May;53(5):449-58. doi: 10.7164/antibiotics.53.449.
WF14865A and B, novel cathepsins B and L inhibitors, were produced and isolated separately from the culture mycelium of a fungal strain Aphanoascus fulvescens No. 14865. Spectroscopic analysis revealed that both WF14865A and B were composed of trans-epoxysuccinyl moieties, 1-H-imidazole-2-ylamine, and isoleucine or leucine. These compounds inhibited human cathepsins B and L with IC50 values in the range of 8.4 approximately 72nM in vitro. Though their in vitro properties were typical as trans-epoxysuccinyl type inhibitors, they exerted strong bone resorption inhibitory effects in low-calcium-diet-fed mouse model at 3.2 approximately 10 mg/kg.

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