UK 356618

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

UK 356618  纯度: 98.91%

UK 356618 (Compound 4j) 是一种有效且选择性的基质金属蛋白酶 3 (MMP-3) 抑制剂,其 IC50 值为 5.9 nM。与 MMP-3相比,UK 356618 对 MMP-1,MMP-2,MMP-9, MMP-13 和 MMP-14 的抑制效力较低。

UK 356618

UK 356618 Chemical Structure

CAS No. : 230961-08-7

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1 mg ¥1700 In-stock
5 mg ¥5100 In-stock
10 mg ¥8700 In-stock
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生物活性

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)

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

557.72

Formula

C34H43N3O4

CAS 号

230961-08-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (44.83 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7930 mL 8.9651 mL 17.9301 mL
5 mM 0.3586 mL 1.7930 mL 3.5860 mL
10 mM 0.1793 mL 0.8965 mL 1.7930 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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.

    [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.

    [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.

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