Marimastat

SKU: orb1300377

Description

Marimastat (BB-2516) is a potent broad-spectrum matrix metalloproteinase (MMP) inhibitor with low nanomolar activity against key enzymes like MMP-9, MMP-1, and MMP-2. It has been widely used in vitro and in vivo to study the role of MMPs in cancer metastasis, angiogenesis, and inflammatory diseases.

Research Area

Cardiovascular Research, Neuroscience

Key Properties

• CAS Number: 154039-60-8
• MW: 331.4
• Purity: >98%
• Formula: C₁₅H₂₉N₃O₅
• SMILES: CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)[C@H](O)C(=O)NO)C(C)(C)C
• Target: Protease
• Solubility: Soluble in DMSO (30 mg/ml)

Bioactivity

• Target IC50:
  MMP14:9 nM|MMP9:3 nM|MMP1:5 nM|MMP7:13 nM|MMP2:6 nM
• In Vivo:
  Marimastat has a favorable pharmacokinetic profile in humans, as it is almost completely absorbed after oral administration, with a high and predictable bioavailability and a half-life of approximately 15 hr (justifying twice a day dosing), making it a much more palatable treatment option for Clinicalal trials than batimastat. Marimastat is rapidly metabolized in rodents, undergoing a very high first-pass effect, making testing of marimastat in rodents difficult, as sustained plasma concentrations in this species are difficult to obtain.
• In Vitro:
  Marimastat (BB-2516) is a broad-spectrum MMPI with an enzyme inhibitory spectrum very similar to batimastat. Marimastat inhibits CD30 shedding in Karpas 299 cells with an IC50 of 1 microM and also inhibits LPS-induced soluble TNF-alpha production in a dose-dependent manner. The enzyme, tumor necrosis factor alpha convertase (TACE), reported to be closely related to matrix metalloproteinases, is responsible for the processing of pro-TNFalpha to TNFalpha and is specifically inhibited by Marimastat with an IC50 of 3.8 nM.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BB-2516; MATT

Compound Identifiers

PubChem CID

119031