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Marimastat

Catalog No. T6885 CAS 154039-60-8

Synonyms: BB2516, KB-R8898, TA2516

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

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Marimastat, CAS 154039-60-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 229.00
50 mg	In stock	$ 382.00
100 mg	In stock	$ 562.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 98.11%

Purity: 97.46%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).
Targets&IC50	MMP1:5 nM, MMP7:13 nM, MMP2:6 nM, MMP9:3 nM, MMP14:9 nM
In vitro	Marimastat (BB-2516) is a broad-spectrum MMPI with an enzyme inhibitory spectrum very similar to batimastat. [1] Marimastat inhibits CD30 shedding in Karpas 299 cells with an IC50 of 1 microM [2] 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.[3]
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. [1]
Kinase Assay	Compounds 1, 2, 7-9 and 11-16 are pre-incubated with MMP-1 or MMP-3 (10 nM) at different concentrations (0-10 μM) in a mixture of Tris-HCl (50 mM, pH 7.5), NaCl (150 mM), CaCl2 (10 mM), NaN3 (0.02%) and Brij-35 (0.05%) for 1 hour at 37°C. Residual activity is measured using the fluorogenic MMP substrate (2 μM) by fluorescence increase (emission at 393 nm and excitation at 325 nm) on a fluorescence plate reader. The data are fitted to the tight binding inhibitor equation: v=[(E-I-k+[(E-I-k)2+4Ek]1/2)/(2E)], where v is the velocity of the reaction, E is the enzyme concentration, I is the initial inhibitor concentration, and k is the apparent inhibition constant, using the software Prism.

Synonyms	BB2516, KB-R8898, TA2516
Molecular Weight	331.41
Formula	C15H29N3O5
CAS No.	154039-60-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33.1 mg/mL (100 mM)

References and Literature

1. Rasmussen HS, et al. Pharmacol Ther. 1997, 75(1), 69-75. 2. auf dem Keller U, et al. Cancer Res. 2010, 70(19), 7562-7569. 3. Ulasov I, et al. Cancer Med.2013, 2(4), 457-467. 4. Sinno M, et al. Stem Cells Dev. 2013, 22(3), 345-358. 5. Maekawa K, et al. Clin Exp Metastasis. 2002, 19(6), 513-518.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Angiogenesis related Compound Library Clinical Compound Library Pediatric Drug Library Immunology/Inflammation Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Marimastat 154039-60-8 Proteases/Proteasome MMP BB-2516 KB-R 8898 TA 2516 inhibit BB2516 TA-2516 Inhibitor KB-R8898 TA2516 BB 2516 KB-R-8898 Matrix metalloproteinases inhibitor

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