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150651-39-1

中文名稱 1-amino-3-(4-methylphenyl)pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile
英文名稱 1-amino-3-(4-methylphenyl)pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile
CAS 150651-39-1
分子式 C20H13N5
分子量 323.35
MOL 文件 150651-39-1.mol
更新日期 2024/12/17 19:35:12
150651-39-1 結(jié)構(gòu)式 150651-39-1 結(jié)構(gòu)式

基本信息

中文別名
化合物IFSP1
1-氨基-3-(對甲苯基)苯并[4,5]咪唑并[1,2-A]吡啶-2,4-二甲腈
英文別名
iFSP1
1-amino-3-(4-methylphenyl)pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile
Pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile, 1-amino-3-(4-methylphenyl)-

物理化學(xué)性質(zhì)

密度1.31±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO:30.0(Max Conc. mg/mL);92.78(Max Conc. mM)
酸度系數(shù)(pKa)2.90±0.50(Predicted)
形態(tài)結(jié)晶固體
顏色Light yellow to yellow

常見問題列表

生物活性
iFSP1 是一種有效的、選擇性的且不依賴谷胱甘肽的 ferroptosis suppressor protein 1 (FSP1/AIFM2) 的抑制劑,EC50值為103 nM。iFSP1 可在過表達(dá)FSP1的GPX4基因敲除的Pfa1細(xì)胞和HT1080細(xì)胞中選擇性誘導(dǎo)鐵死亡。
靶點(diǎn)
TargetValue
FSP1/AIFM2
(Cell-free assay)
103 nM(EC50)
體外研究

iFSP1 (0.001-1 μM; 24 hours) inhibits the Gpx4-knockout cell growth as a dose-dependent manner, but does not inhibit the wild type cell growth. Treatment with the ferroptosis inhibitor Lip-1 protects GPX4- knockout cells from iFSP1-induced ferroptosis.iFSP1 (0.001-1 μM; 24 hours) is less efficient than genetic deletion of?FSP1, whereas iFSP1 treatment in the?FSP1-knockout background had no additive effect to RSL3-induced?ferroptosis.iFSP1 (3 μM; 24 hours) treatment results in an obvious toxicity of RSL3 in a panel of genetically engineered (FSP1-knockout) human cancer cell lines.AIFM2: the flavoprotein apoptosis-inducing factor mitochondria-associated 2 is a previously unrecognized anti-ferroptotic gene. AIFM2, which is renamed ferroptosis suppressor protein 1 (FSP1)

Cell Proliferation Assay

Cell Line: Wild-type and?Gpx4-knockout Pfa1 or HT 1080 cells overexpressing FSP1–HA
Concentration: 0.001-1 μM
Incubation Time: 24 hours
Result: Was toxic to cells that depend solely (no GPX4 expression detectable) on FSP1 function.

Cell Viability Assay

Cell Line: NCl-H1437, NCl-H1437 FSP1 KO, U-373, U-373 FSP1 KO, MDA-MB-436, MDA-MB-436 FSP1 KO, SW620, SW620 FSP1 KO, MDA-MB-435S, MDA-MB-435S FSP1 KO, A549 and A549 FSP1 KO
Concentration: 3 μM
Incubation Time: 24 hours
Result: Sensitized a variety of human cancer cell lines to the ferroptosis inducer (1S,3R)-RSL3.
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