1. Metabolic Enzyme/Protease
  2. MMP
  3. UK-370106

UK-370106 

Cat. No.: HY-107639 Purity: ≥95.0%
Handling Instructions

UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro.

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

UK-370106 Chemical Structure

UK-370106 Chemical Structure

CAS No. : 230961-21-4

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1 mg USD 160 In-stock
Estimated Time of Arrival: December 31
5 mg USD 470 Get quote
10 mg USD 800 Get quote
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro[1][2].

IC50 & Target[1][2]

MMP-3

23 nM (IC50)

MMP-12

42 nM (IC50)

MMP-8

1.75 μM (IC50)

MMP-13

2.3 μM (IC50)

MMP-7

5.8 μM (IC50)

MMP-9

30.4 μM (IC50)

MMP-2

34.2 μM (IC50)

MMP-14

66.9 μM (IC50)

In Vitro

The potency of UK-370106 (compound 7) for the inhibition of MMP-13 is 2.3 µM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC50 > 100 µM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC50 of 34.2 µM), MMP-7 (IC50 of 5.8 µM), MMP-8 (IC50 of 1.75 µM), MMP-9 (IC50 of 30.4 µM) and MMP-14 (IC50 of 66.9 µM)[1].
UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) but does not inhibit cleavage of [3H]-gelatin by either MMP-2 or -9 up to the highest concentration tested (100 µM)[1].
UK-370106 is not cytotoxic to, nor affected proliferation of, fibroblasts, keratinocytes, or endothelial cells at 50-100 µM in vitro[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Following iv (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is cleared rapidly (t1/2 = 23 min) from plasma, but slowly (t1/2 approximately 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

572.73

Formula

C₃₅H₄₄N₂O₅

CAS No.
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
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (349.20 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7460 mL 8.7301 mL 17.4602 mL
5 mM 0.3492 mL 1.7460 mL 3.4920 mL
10 mM 0.1746 mL 0.8730 mL 1.7460 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (8.73 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (8.73 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (8.73 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: ≥99.0%

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Product Name:
UK-370106
Cat. No.:
HY-107639
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