Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is aHIVfusion inhibitor withED₅₀s of 0.05 to 5.7 μM for acuteHIVtype 1 (HIV-1) andHIV-2infections. Siamycin I inhibits thegelatinaseand gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, anantibiotic, has the potential for enterococcal infections research^[1][2][3][4].

Siamycin I 浓度为 1 μM 轻微抑制E. faecalis的生长 (接种后 5 小时生长 80%)，浓度为 5 μM 时完全抑制生长 (接种后 12 小时无生长)^[3]。
siamycin I (0-1 μM; 24 小时) 在 0.25 μM 浓度下轻微抑制生物膜形成，浓度高于 0.5 μM 时抑制作用显着^[3]。
Siamycin I 抑制 C8166 细胞与慢性感染 HIV 的 CEM-SS 细胞之间的融合 (ED₅₀=0.08 μM)，但对 Sendai 病毒诱导的融合或小鼠成肌细胞融合没有影响^[4]。

2163.48

C₉₇H₁₃₁N₂₃O₂₆S₄

164802-68-0

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