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Amastatin, also known as 3-amino-2-hydroxy-5-methylhexanoyl-L-valyl-L-valyl-L-aspartic acid, is a naturally occurring, competitive and reversible aminopeptidase inhibitor. Amastatin has originally been isolated from the culture filtrate of Streptomyces sp. ME98-M3 and is a competitive inhibitor of human serum aminopeptidase A (Ki = 1.1 · 10⁻⁶ M) and of pig kidney leucine aminopeptidase (Ki = 1.6 · 10⁻⁶ M). Amastatin hydrochloride has been shown to slightly decrease the conversion of angiontensin II to angiotensin III, but significantly increases the potency of angiotensin III and des(Asp1)angiotensin I.
