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4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-

4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-

中文名稱4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
中文同義詞6-甲基-2-((2-(萘-1-基)-2-氧代乙基)硫基)嘧啶-4(3H)-酮;化合物I3MT-3;化合物I3MT-3,10 MM DMSO 溶液;I3MT-3 ,S3541
英文名稱4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
英文同義詞4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-;I3MT-3;13MT-3;6-Methyl-2-((2-(naphthalen-1-yl)-2-oxoethyl)thio)pyrimidin-4(3H)-one;6-Methyl-2-((2-(naphthalen-1-yl)-2-oxoethyl)thio)pyrimidin-4(3H)-one[I3MT-3;HMPSNE;EA.hy926 cells,Hippo (MST),inhibit,I3MT-3,3MST,HEK293,I3MT3,cell-membrane,COS-7,I-3MT-3,I3MT 3,Inhibitor;I3MT-3, 10 mM in DMSO
CAS號459420-09-8
分子式C17H14N2O2S
分子量310.37
EINECS號
相關(guān)類別
Mol文件459420-09-8.mol
結(jié)構(gòu)式4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]- 結(jié)構(gòu)式

4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]- 性質(zhì)

沸點514.9±52.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
儲存條件Store at -20°C
溶解度二甲基亞砜:125 mg/mL(402.75 mM)
酸度系數(shù)(pKa)7.72±0.50(Predicted)
形態(tài)固體
顏色米白色至淺棕色

4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]- 用途與合成方法

I3MT-3 (HMPSNE) 是有效、選擇性和具有細(xì)胞膜滲透性的 3-巰基丙酮酸硫轉(zhuǎn)移酶 (3MST) (IC50=2.7 μM) 的抑制劑,對其他硫化氫/磺胺制硫酶沒有活性。I3MT-3 靶向位于 3MST 活性位點的過硫半胱氨酸殘基。

IC50: 2.7 μM (3-Mercaptopyruvate sulfurtransferase (3MST))

I3MT-3 (1?μM) is selective for 3MST and shows a high inhibitory activity (80–90%) even at 10?μM in cell lysate of 3MST-overexpressing HEK293 cells. Besides, it is almost inactive towards the other two H2S-producing enzymes even at 100 μM. I3MT-3 (1?μM) 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 IC 50 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 IC 50 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 IC 50 of approximately 30 μM).I3MT-3 (0-300 μM; 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 (0-300 μM; 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: 0 μM; 10 μM; 30 μM; 100 μM; 300 μM
Incubation Time: 48 hours
Result: Slowed down proliferation of CT26 cells.

安全信息

MSDS信息

更新日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/07/06S35414(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
I3MT-3
459420-09-85mg2039.87元
2026/07/06S35414(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
I3MT-3
459420-09-825mg6117.98元

4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]- 上下游產(chǎn)品信息

"4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-"相關(guān)產(chǎn)品信息
4(3H)-Pyrimidinone,6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
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