GPX4-IN-3

• CAT Number: I045235
• CAS Number: 2761004-85-5
• Molecular Formula: C29H24ClN3O3S
• Molecular Weight: 530.04
• Purity: ≥95%
• Synonyms: 2-(1-benzothiophen-3-yl)-2-[N-(2-chloroacetyl)-4-(1,3-oxazol-5-yl)anilino]-N-(2-phenylethyl)acetamide
• InChI: InChI=1S/C29H24ClN3O3S/c30-16-27(34)33(22-12-10-21(11-13-22)25-17-31-19-36-25)28(24-18-37-26-9-5-4-8-23(24)26)29(35)32-15-14-20-6-2-1-3-7-20/h1-13,17-19,28H,14-16H2,(H,32,35)
• InChIKey: ZLCPSXKEQBUXRJ-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)CCNC(=O)C(C2=CSC3=CC=CC=C32)N(C4=CC=C(C=C4)C5=CN=CO5)C(=O)CCl

GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM[1].
GPX4-IN-3 (26a) exhibits IC50 values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively[1].
GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3[1].
GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity[1].
GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity[1].
GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1)[1].
GPX4-IN-3 (26a) exertes antitumor activity and good biological safety in vivo[1].

Reference

[1]. Congjun Xu, et al. Discovery of a Potent Glutathione Peroxidase 4 Inhibitor as a Selective Ferroptosis Inducer. J Med Chem. 2021 Sep 23;64(18):13312-13326.
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