Cas No.: | 150651-39-1 |
SMILES: | CC1=CC=C(C=C1)C2=C(C3=NC4=CC=CC=C4N3C(=C2C#N)N)C#N |
Formula: | C20H13N5 |
M.Wt: | 323.35 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [1]. Doll S, et al. FSP1 is a glutathione-independent ferroptosis suppressor.Nature. 2019 Nov;575(7784):693-698. |
Description: | iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A)[1]. |
Target: | EC50: 103 nM (FSP1)[1] |
In Vitro: | 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[1]. 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[1]. 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[1]. 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)[1] Cell Proliferation Assay[1] 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[1] 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. |
References: | [1]. Doll S, et al. FSP1 is a glutathione-independent ferroptosis suppressor.Nature. 2019 Nov;575(7784):693-698. |