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Synonyms: UK-356618, UK356618

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 5 mg | $971 | 35 days | 35 days | |
| 10 mg | $1,400 | 35 days | 35 days | |
| 25 mg | $2,260 | 35 days | 35 days |
| Description | UK 356618 is a potent and selective matrix metalloproteinase 3 (MMP-3) inhibitor with an IC50 of 5.9 nM. Its inhibitory activities against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 are all weaker than that against MMP-3. |
| Targets & IC50 | MMP2:1.79 μM, MMP14:1.9 μM, MMP13:73 nM, MMP1:51 μM, MMP9:0.84 μM, MMP3:5.9 nM |
| In vitro | Methods: In vitro cell experiments and molecular interaction studies were performed to explore the effects of substituent size on MMP‑3 inhibitory activity and MMP‑2 selectivity, as well as the pharmacological characteristics of UK 356618 against MMPs and its effect on TNF‑α‑induced lung cancer cell migration. Results: : 1.The inhibitory activity against MMP‑3 and the selectivity for matrix metalloproteinase 2 (MMP‑2) were highly sensitive to substituent size, among which methyl substitution showed the optimal effect (corresponding compound UK 356618). Compared with other matrix metalloproteinases (MMPs), UK 356618 exhibited a broader spectrum of action [1]. 2.MMP‑13 is closely associated with tumor metastasis‑related interleukin‑6 (IL‑6) and tumor necrosis factor‑α (TNF‑α). MMP‑13 knockout abolished the promotive effect of TNF‑α on lung cancer cell migration, and treatment with UK 356618 also effectively blocked the migration of NCI‑H446 lung cancer cells induced by TNF‑α [2]. |
| In vivo | Methods: Male Wistar rats were intravenously administered UK 356618 at a dose of 15 mg/kg. Reperfusion was performed at 24 hours and 7 days after administration, and the effect on MMP3 activity in the rat brain was detected. Results: After intravenous injection of UK 356618 at 15 mg/kg followed by reperfusion at 24 hours and 7 days respectively, MMP3 activity in the brain of male Wistar rats was significantly reduced [3]. |
| Synonyms | UK-356618, UK356618 |
| Molecular Weight | 557.72 |
| Formula | C34H43N3O4 |
| Cas No. | 230961-08-7 |
| Smiles | CC1=C(C=CC(CCC[C@@H](C(N[C@H](C(N[C@H](C)C2=CC=CC=C2)=O)[C@@](C)(C)C)=O)CC(NO)=O)=C1)C3=CC=CC=C3 |
| Relative Density. | 1.124 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 20 mg/mL (35.86 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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