Батимастат

Использование

Batimastat has been used to inhibit matrix metalloproteinases (MMPs) activity in various studies.

Общее описание

A Marimastat (Cat. No. 444289) type of peptidyl hydroxamate-based inhibitor that potently inhibits a broad-spectrum of metalloproteinases, including MMP-1, MMP-2, MMP-3/stromelysin, MMP-7/matrilysin, MMP-9, ΔMT1 (MMP-14 without TM domain), ADAM8, and ADAM17/TACE (IC₅₀ = 3, 4, 20, 6, 4, 2.08, 51.3, and 19 nM, respectively), by targeting both the substrate binding site and the active-site Zn²⁺, while being much less potent toward ACE (Angiotensin Converting Enzyme) or α-secretase (IC₅₀ = 1.6 and 3.3 μM, respectively). Batimastat is widely used in studying the involvement of MMPs in cancinogenesis and non-cancer pathological processes both in cultures in vitro and in animals in vivo.

Биологическая активность

Potent, broad spectrum matrix metalloprotease (MMP) inhibitor (IC 50 values are 3, 4, 4, 6 and 20 nM for MMP -1, -2, -9, -7 and -3 respectively). Exhibits antiproliferative, anti-invasive and antimetastatic activity in human ovarian carcinoma xenografts in vivo .

Ферментативный ингибитор

This potent, broad-spectrum matrix metalloprotease, or MMP, inhibitor (FW = 477.64 g/mol; CAS 130370-60-4; Solubility: 96 mg/mL DMSO, <1 mg/mL H2O), also known by its code name BB-94 and its systematic name (2R,3S)-N4 -hydroxy-N1 -[(1S)-2-(methylamino)-2-oxo-1-(phenylmethyl) ethyl]-2-(2-methylpropyl)-3-[(2-thienylthio)methyl]butanediamide, targets MMP-1 (IC50 = 3 nM), MMP-2 (IC50 = 4 nM), MMP-9 (IC50 = 4 nM), MMP-7 (IC50 = 6 nM) and MMP-3 (IC50 = 22 nM). Matrix metalloproteinases have been implicated in the growth and spread of metastatic tumors, and Batimastat not only prevents colonization of secondary organs by B16-BL6 cells, but limits the growth of solid tumors. Animals receiving BB-94 (30 mg/kg, i.p., once daily for 60 days, followed by 3 times weekly) show a reduction in the median primary tumor weight from 293 mg in the control group to 144 mg in the treated group. BB-94 treatment also reduces the incidence of local and regional invasion. Batimastat also reduces in vivo growth of experimental hemangiomas, most probably by blocking endothelial cell recruitment by the transformed cells or by interfering with cell organization in vascular structures. Target(s): Trimeresurus mucrosquamatus (Taiwan habu) venom metalloproteinases; matrix metalloproteinases; interstitial collagenase, or MMP1; stromelysin, or MMP3; matrilysin, or MMP7; gelatinase A, or or MMP2; gelatinase B, or or MMP9; neutrophil collagenase, or MMP8; atrolysin C, or Crotalus atrox metalloendopeptidase c; membrane-type 1 matrix metalloproteinase, or MMP14; membrane-type 3 matrix metalloproteinase, or MMP-16; ADAM 17 endopeptidase, or tumor necrosis factor-a converting enzyme; TACE (13- 15); a-secretase; ADAM TS-4 endopeptidase, or aggrecanase; macrophage elastase, or MMP12.