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459420-09-8

中文名稱 4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
英文名稱 4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-
CAS 459420-09-8
分子式 C17H14N2O2S
分子量 310.37
MOL 文件 459420-09-8.mol
更新日期 2023/03/20 15:41:25
459420-09-8 結(jié)構(gòu)式 459420-09-8 結(jié)構(gòu)式

基本信息

中文別名
化合物I3MT-3
6-甲基-2-((2-(萘-1-基)-2-氧代乙基)硫基)嘧啶-4(3H)-酮
英文別名
13MT-3
I3MT-3
4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-

物理化學性質(zhì)

沸點514.9±52.0 °C(Predicted)
密度1.30±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 125 mg/mL (402.75 mM)
酸度系數(shù)(pKa)7.72±0.50(Predicted)
形態(tài)Solid
顏色Off-white to light brown

安全數(shù)據(jù)

危險性符號(GHS)有害 (GHS07)
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-價格(試劑級)
報價日期產(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
2026/06/05HY-128206I3MT-3459420-09-81 mg840元

常見問題列表

生物活性
I3MT-3 (HMPSNE) 是有效、選擇性和具有細胞膜滲透性的 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。
靶點

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

體外研究

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.
"459420-09-8" 相關(guān)產(chǎn)品信息
459420-09-8 119730-10-8
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