1. Metabolic Enzyme/Protease
  2. MMP
  3. UK 356618

UK 356618 

Cat. No.: HY-107394 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

UK 356618 Chemical Structure

UK 356618 Chemical Structure

CAS No. : 230961-08-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 442 In-stock
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 Get quote
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Based on 1 publication(s) in Google Scholar

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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[1].

IC50 & Target[1][2]

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)

In Vitro

Inhibition of MMP-3 and selectivity over MMP-2 was remarkably sensitive to the size of the substituent and is clearly optimal for a methyl group (UK 356618, compound 4j). 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].

Animal Model: Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO)[3]
Dosage: 15 mg/kg
Administration: Intravenous injection; for 24 h or 7 days
Result: Significantly reduced MMP3 activity in the brain.
Molecular Weight

557.72

Formula

C₃₄H₄₃N₃O₄

CAS No.

230961-08-7

SMILES

CC1=C(C2=CC=CC=C2)C=CC(CCC[[email protected]](CC(NO)=O)C(N[[email protected]@H](C(C)(C)C)C(N[[email protected]@H](C3=CC=CC=C3)C)=O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: >98.0%

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Keywords:

UK 356618UK356618UK-356618MMPMatrix metalloproteinasesReperfusionhyperglycemicTNF-αmigrationcellInhibitorinhibitorinhibit

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UK 356618
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HY-107394
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