中文名称: I3MT-3
英文名称: I3MT-3
CAS No: 459420-09-8
分子式: C17H14N2O2S
分子量: 310.371
I10427 I3MT-3 ≥98% (psaitong)
包装规格:
10mg 25mg 50mg in glass bottle
溶解性:
溶于DMSO(100mg/mL超声)
产品描述:

基本信息

产品编号:

I10427 

产品名称:

I3MT-3

CAS:

459420-09-8

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C17H14N2O2S

溶于液体

-80℃

两年

分子量

310.37

-20℃

1个月

化学名: 

6-Methyl-2-((2-(naphthalen-1-yl)-2-oxoethyl)thio)pyrimidin-4(3H)-one

Solubility (25°C):

 

体外:

 

DMSO

62 mg/mL (199.76mM)

Ethanol

2 mg/mL (6.44mM)

Water

Insoluble

体内(现配现用):

 

1mg/ml表示微溶或不溶。

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。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

3.2220mL

16.1098mL

32.2196mL

5mM

0.6444mL

3.2220mL

6.4439mL

10mM

0.3222mL

1.6110mL

3.2220mL

50mM

0.0644mL

0.3222mL

0.6444mL

 

生物活性

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。

靶点

3MST 
(Cell-free assay)

2.7μM

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

Cell Line:

CT26 cells

Concentration:

0μM; 10μM; 30μM; 100μM; 300μM

Incubation Time:

48 hours

Result:

Slowed down proliferation of CT26 cells.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

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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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

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  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):