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MedChemExpressModel UK 356618 -230961-08-7

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UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is less potent against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 compared with MMP-3[1].
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UK 356618

MCE China:UK 356618

Brand:MedChemExpress (MCE)

Cat. No.HY-107394

CAS:230961-08-7

Purity:98.51%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is less potent against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 compared with MMP-3.

In Vitro:UK 356618 is more widely profiled against other MMPs[1]. MMP-13 is closely involved in IL-6 or TNF-α increasing tumor metastasis. MMP-13 deficiency abrogate TNF-α effect on lung cancer cell migration. UK 356618 treatment efficiently abolished the effect of TNF-α on cell migration in NCI-H446 cells[2].

In Vivo:UK 356618 (15 mg/kg; intravenous injection; for 24 h or 7 days; male Wistar rats) treatment at reperfusion significantly reduces MMP3 activity in the brain[3].

IC50 & Target:MMP-3 5.9 nM (IC50) MMP-13 73 nM (IC50) MMP-9 0.84 μM (IC50) MMP-2 1.79 μM (IC50) MMP-14 1.9 μM (IC50) MMP-1 51 μM (IC50)

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References:

[1]. Fray MJ, et al. Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1). Bioorg Med Chem Lett. 2001 Feb 26;11(4):571-4.  [Content Brief]

[2]. Yan HQ, et al. Ataxia-telangiectasia mutated activation mediates tumor necrosis factor-alpha induced MMP-13 up-regulation and metastasis in lung cancer cells. Oncotarget. 2016 Sep 20;7(38):62070-62083.  [Content Brief]

[3]. Hafez S, et al. Matrix Metalloprotease 3 Exacerbates Hemorrhagic Transformation and Worsens Functional Outcomes in Hyperglycemic Stroke. Stroke. 2016 Mar;47(3):843-51.  [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
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•   The biological activity of the products has been verified by the experiments of customers in various countries;
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
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