Marimastat (BB-2516)

製品コードS7156 バッチS715602

印刷

化学情報

Chemical Structure Synonyms TA2516 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H29N3O5
分子量 331.41 CAS No. 154039-60-8
Solubility (25°C)* 体外 DMSO 54 mg/mL (162.94 mM)
Ethanol (warmed with 50ºC water bath) 7 mg/mL (21.12 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Marimastat (BB-2516, TA2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.
in vitro

Marimastat (BB-2516) (100 nM) significantly inhibits the expression of MMP14 in U251, U87, GBM39, and GBM43 tumor cells. This compound specifically inhibits the growth of glioma cells and has no effect on normal human astrocytes (NHA).[3]

It early down-regulates the expression of Notch target genes, such as Hes1 and Hes5.[4]
in vivo

In an orthotopic oral squamous cell carcinoma implantation model, Marimastat (BB-2516) (150 mg/kg/day, p.o.) administered by an osmotic pump significantly suppresses the cervical lymph node metastasis and activation of MMP-2, and has a significantly better survival than control group.[5]

This compound reduces MMP hyperactivity of polycystic human and rat cholangiocytes and blocks the cystic expansion of PCK cholangiocytes. Chronic treatment of 8-week-old PCK rats with it inhibits hepatic cystogenesis and fibrosis.[6]

プロトコル(参考用のみ)

キナーゼアッセイ Inhibitor kinetics
Recombinant human MMP2 is activated with 1 mM of 4-aminophenylmercuric acetate for 1 hour at 37°C. Rates of cleavage of 1 μM of the quenched fluorescent MMP substrate (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-[3-(2,4-dinitrophenyl)-L-2,3-diaminoproprionyl]-Ala-Arg-NH2 are measured in 96-well fluorimetry plates at 37°C 100 mM Tris-HCl (pH 7.5), 100 mM NaCl, 10 mM CaCl2, 0.05% Brij 35 using a 320 nm excitation filter and a 405 nm emission filter in the presence of increasing concentrations of Marimastat (BB-2516). Curve-fitting and IC50 calculations are done using GraphPad Prism 5.0 Software.
細胞アッセイ 細胞株 U251, U87, GBM39, and GBM43 cell lines
濃度 100 nM
反応時間
実験の流れ

At selected time points, cell proliferation is measured by MTT assay by adding 20 μL of MTT substrate to each well. After 3 h of incubation at 37 ° C and 5% CO2, 100 μL of sodiumdodecyl sulphate (SDS)-based stop solution is added to each well to stop the enzymatic reaction. On the following day, the absorbance is measured by the Multiscan MS microplate reader with a reference at 650 serving as a blank.
動物実験 動物モデル Orthotopic oral squamous cell carcinoma implantation model
投薬量 150 mg/kg/day
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/9364582/
  • https://pubmed.ncbi.nlm.nih.gov/20729277/
  • https://pubmed.ncbi.nlm.nih.gov/24156018/
  • https://pubmed.ncbi.nlm.nih.gov/23098139/
  • https://pubmed.ncbi.nlm.nih.gov/12405288/
  • https://pubmed.ncbi.nlm.nih.gov/24436140/

カスタマーフィードバック

Data from [Data independently produced by , , Cell Signal, 2018, 42:155-164]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

ERK activation waves coordinate mechanical cell competition leading to collective elimination via extrusion of bacterially infected cells [ Cell Rep, 2025, 44(1):115193] PubMed: 39817903
Evaluating therapeutic plasma exchange and protease inhibitors as mechanisms to reduce soluble mesothelin [ Sci Rep, 2025, 15(1):13174] PubMed: 40240561
Oncogenic EML4-ALK assemblies suppress growth factor perception and modulate drug tolerance [ Nat Commun, 2024, 15(1):9473] PubMed: 39488530
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
Targeting the core program of metastasis with a novel drug combination [ Cancer Med, 2024, 13(11):e7291] PubMed: 38826119
CD26-negative and CD26-positive tissue-resident fibroblasts contribute to functionally distinct CAF subpopulations in breast cancer [ Nat Commun, 2023, 14(1):183] PubMed: 36635273
Chronic kidney disease causes blood-brain barrier breakdown via urea-activated matrix metalloproteinase-2 and insolubility of tau protein [ Aging (Albany NY), 2023, 15(20):10972-10995] PubMed: 37889501
Cell-matrix interface regulates dormancy in human colon cancer stem cells [ Nature, 2022, 10.1038/s41586-022-05043-y] PubMed: 35798028
Hotspot ESR1 mutations are multimodal and contextual modulators of breast cancer metastasis [ Cancer Res, 2022, canres.CAN-21-2576-E.2021] PubMed: 35078818
Transforming growth factor β1 signaling links extracellular matrix remodeling to intracellular lipogenesis upon physiological feeding events [ J Biol Chem, 2022, 298(4):101748] PubMed: 35189145

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。