To overcome the problem of frequent isolation of known compounds in actinomycete drug discovery, sequence-based strain selection was employed. A Streptomyces strain TP-A0874, isolated from a compost sample in Ishikawa, Japan, and sharing 96.3% 16S rRNA gene identity with S. albus, was found to produce a new catecholate derivative, catechoserine (1), along with two known biosynthetically related metabolites, N,N¢-bis(2,3-dihydroxybenzoyl)-O-L-seryl L-serine (2) and N,N¢,N¢-tris(2,3-dihydroxybenzoyl)-O-L-seryl-O-L-seryl L-serine (3). The whole culture broth of TP-A0874 was separated into supernatant and mycelium; the mycelium was extracted with methanol, and the combined aqueous solution was fractionated by HP-20 resin column chromatography and purified by reversed-phase HPLC to yield compounds 1–3. Catechoserine (1) was characterized as a colorless amorphous solid with molecular formula C14H19NO6 (HR-ESITOFMS: obsd (M+Na)+ m/z 320.1101). Its structure was determined by IR (hydroxyl, carbonyl), UV (hydroxylated benzoyl chromophore), NMR (1H, 13C, 2D NMR), and Marfey's analysis (L-configuration of serine). Compounds 1–3 were evaluated in a tumor cell invasion assay using Matrigel. Compound 1 inhibited invasion of murine colon carcinoma 26-L5 cells with an IC50 of 2.5 μM, while 2 and 3 had IC50 values of 2.7 and 5.8 μM, respectively. They did not inhibit adhesion, extracellular matrix degradation, or migration at 1–10 μM and showed no antimicrobial activity against Micrococcus luteus, Escherichia coli, or Candida albicans (MICs > 30 mg ml-1). Compounds 2 and 3 are partially degraded products of enterobactin, and this is the first report of their antiinvasive activities. The simple structural units of these compounds provide a starting point for optimizing new antiinvasive agents through analog synthesis.