Marimastat (BB-2516)

製品コードS7156 バッチS715602

化学情報

	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	7 mg/mL warmed with 50ºC water bath (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.

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 (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]

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 (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]

プロトコル(参考用のみ)

キナーゼアッセイ	Inhibitor kinetics
キナーゼアッセイ	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 inhibitor concentrations. 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

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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：

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
Transcriptional networks identify synaptotagmin-like 3 as a regulator of cortical neuronal migration during early neurodevelopment [ Cell Rep, 2021, 34(9):108802]	PubMed: 33657377

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。

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