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UK 370106

Catalog No.
A4441
MMP-3/MMP-12 Inhiibitor,highly selective
Grouped product items
SizePriceStock Qty
10mg
$636.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 23 nm (MMP-3)

Stromelysin-1 also known as matrix metalloproteinase-3 (MMP-3) is an enzyme that in humans is encoded by the MMP3 gene. Proteins of the matrix metalloproteinase (MMP) family are involved in the breakdown of extracellular matrix and during tissue remodeling in normal physiological processes, such as embryonic development and reproduction, as well as in disease processes, such as arthritis, and tumour metastasis (http://en.wikipedia.org/wiki/MMP-3).

In vitro: UK-370106, a potent inhibitor of MMP-3 (IC50 ) 23 nM) with >1200-fold weaker potency vs MMP-1, -2, -9, and -14. MMP-13, may contribute to the pathology of chronic wounds. UK-370106 potently inhibited cleavage of [3H]-fibronectin by MMP-3 (IC50 ) 320 nM) but not cleavage of [3H]-gelatin by either MMP-2 or -9 (up to 100 íM). UK-370106 had little effect, at MMP-3 selective concentrations, on keratinocyte migration over a collagen matrix in vitro, which is a model of the re-epithelialization process [1].

In vivo: Following iv (rat) or topical administration to dermal wounds (rabbit), UK-370106 was cleared rapidly (t1/2=23 min) from plasma, but slowly (t1/2 ~ 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibited MMP-3 ex vivo. These data suggest UK-370106 is sufficiently potent to inhibit MMP-3-mediated matrix degradation while leaving unaffected cellular migration mediated by MMPs 1, 2, and 9. These properties make UK-370106 a suitable candidate for progression to clinical trials in human chronic dermal wounds, such as venous ulcers [1].

Clinical trial: Pfizer described the discovery of UK-370106, a highly selective peptidicMMP-3 inhibitor, which was identified as a clinical candidate for the topical treatment of chronic dermal ulcers [2], however, it is now still in the preclinical stage and no clinical trial is ongoing.

References:
[1] Fray MJ, Dickinson RP, Huggins JP, Occleston NL.  A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003;46(16):3514-25.
[2] Whitlock GA, Dack KN, Dickinson RP, Lewis ML.  A novel series of highly selective inhibitors of MMP-3. Bioorg Med Chem Lett. 2007;17(24):6750-3.

Product Citation

Chemical Properties

Physical AppearanceWhite solid
StorageStore at 4°C
M.Wt572.73
Cas No.230961-21-4
FormulaC35H44N2O5
Solubility<57.27mg/ml in DMSO; <14.32mg/ml in ethanol
Chemical Name(3R)-3-[[(2S)-1-[[(1S)-2-methoxy-1-phenylethyl]amino]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]-6-(3-methyl-4-phenylphenyl)hexanoic acid
SDFDownload SDF
Canonical SMILESCC1=C(C=CC(=C1)CCCC(CC(=O)O)C(=O)NC(C(=O)NC(COC)C2=CC=CC=C2)C(C)(C)C)C3=CC=CC=C3
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description UK 370106 is a highly selective inhibitor of MMP-3 and MMP-12 with IC50 values of 23 nM and 42 nM, respectively.
Targets MMP-3 MMP-12 MMP-8 MMP-13 MMP-7 MMP-9
IC50 23 nM 42 nM 1.75 μM 2.3 μM 5.8 μM 30.4 μM

Quality Control

Quality Control & MSDS

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Chemical structure

UK 370106

Related Biological Data

UK 370106