Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Formula | C15H29N3O5 |
|||
Molecular Weight | 331.41 | CAS No. | 154039-60-8 | |
Solubility (25°C)* | In vitro | DMSO | 54 mg/mL (162.94 mM) | |
Ethanol | 7 mg/mL (21.12 mM) | |||
Water | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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. | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Targets |
|
|||||||||||
In vitro | Marimastat (100 nM) significantly inhibits the expression of MMP14 in U251, U87, GBM39, and GBM43 tumor cells. Marimastat specifically inhibits the growth of glioma cells and has no effect on normal human astrocytes (NHA).[3] Marimastat 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 (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] Marimastat 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 marimastat inhibits hepatic cystogenesis and fibrosis.[6] |
Kinase Assay: |
|
---|---|
Animal Study: |
|
Data from [Data independently produced by , , Cell Signal, 2018, 42:155-164]
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 |
Evaluation of the matrix metalloproteinase 9 (MMP9) inhibitor Andecaliximab as an Anti-invasive therapeutic in Head and neck squamous cell carcinoma [ Oral Oncol, 2022, 132:106008] | PubMed: 35803110 |
Marimastat alleviates oxidative stress induced cellular senescence by activating autophagy [ Biochem Biophys Res Commun, 2022, 620:121-128] | PubMed: 35780580 |
Lymphocyte access to lymphoma is impaired by high endothelial venule regression [ Cell Rep, 2021, 37(4):109878] | PubMed: 34706240 |
EPB41L5 controls podocyte extracellular matrix assembly by adhesome-dependent force transmission [ Cell Rep, 2021, 34(12):108883] | PubMed: 33761352 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.