| 中文名称: | I3MT-3 | ||||
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| 英文名称: | I3MT-3 | ||||
| 别名: | HMPSNE 6-Methyl-2-((2-(naphthalen-1-yl)-2-oxoethyl)thio)pyrimidin-4(3H)-one | ||||
| CAS No: | 459420-09-8 | 分子式: | C17H14N2O2S | 分子量: | 310.371 |
| CAS No: | 459420-09-8 | ||||
| 分子式: | C17H14N2O2S | ||||
| 分子量: | 310.371 | ||||
基本信息
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产品编号： |
I10427 |
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产品名称： |
I3MT-3 |
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CAS: |
459420-09-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
310.37 |
-20℃ |
1个月 |
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化学名： |
6-Methyl-2-((2-(naphthalen-1-yl)-2-oxoethyl)thio)pyrimidin-4(3H)-one |
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Solubility (25°C)： |
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体外:
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DMSO |
62 mg/mL (199.76mM) |
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Ethanol |
2 mg/mL (6.44mM) |
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Water |
Insoluble |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.2220mL |
16.1098mL |
32.2196mL |
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5mM |
0.6444mL |
3.2220mL |
6.4439mL |
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10mM |
0.3222mL |
1.6110mL |
3.2220mL |
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50mM |
0.0644mL |
0.3222mL |
0.6444mL |
生物活性
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产品描述 |
一种有效、选择性和具有细胞膜渗透性的 3-巯基丙酮酸硫转移酶 (3MST) (IC50=2.7μM) 的抑制剂，对其他硫化氢/磺胺制硫酶没有活性。I3MT-3 靶向位于 3MST 活性位点的过硫半胱氨酸残基。 |
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靶点 |
3MST |
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2.7μM |
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体外研究 |
I3MT-3 (1μM) is selective for 3MST and shows a high inhibitory activity (80–90%) even at 10μM in cell lysate of 3MSToverexpressing HEK293 cells. Besides, it is almost inactive towards the other two H2S-producing enzymes even at 100μM . I3MT-3 (1μM) shows a high selectivity for 3MST, it completely suppresses the 3MST activity in COS7 cells living cells. I3MT-3 produces a concentration-dependent inhibition of the AzMC (the fluorescent H2S probe) signal when incubated with purified human recombinant enzyme, the inhibition of the catalytic activity of 3-MST produces a concentration-dependent inhibition of H2S production with an IC50 of 13.6 µM. I3MT-3 shows a dose-dependent inhibition of 3-MST activity from CT26 homogenates, which contain the murine form of the enzyme. The IC50 of HMPSNE for murine 3-MST is calculated as 2.3 µM with a cozncentration-dependent decrease of AzMC fluorescence . I3MT-3 (10 µM-100 µM; after 3 h probe AzMC) causes a partial inhibition of the signal, while at 100 µM, HMPSNE causes a complete inhibition of the AzMC-guided H2S fluorescence at 100 µM, Additionally, HMPSNE is capable of inhibiting its target in situ in CT26 cells (with an IC50 of approximately 30 µM). I3MT-3 (0-300μM; 5-50 hours) does not enhance MTT conversion at 10 µM, while at 100 and 300 µM it produces an inhibitory response, without increasing the LDH signal, i.e., without inducing any detectable degree of cell necrosis. It also produces a decreased oxygen consumption rate (OCR) profiles in CT26 cells . I3MT-3 (0-300μM; 48 hours) inhibits CT26 cells proliferate with increasing concentrations of I3MT-3. Confluence of cells treated with HMPSNE is recorded each hour for 48 h by the IncuCyte method. Cell Proliferation Assay |
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Cell Line: |
CT26 cells |
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Concentration: |
0μM; 10μM; 30μM; 100μM; 300μM |
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Incubation Time: |
48 hours |
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Result: |
Slowed down proliferation of CT26 cells. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
