SGC3027

**SGC3027** is a potent, selective, and cell-active chemical probe that acts as a prodrug of SGC8158, a SAM-competitive inhibitor of protein arginine methyltransferase 7 (**PRMT7**) with an IC₅₀ below 2.5 nM for methylation of histone H2B (residues 23-37). Developed through a collaboration between the **Structural Genomics Consortium (SGC)**, **Takeda**, and the **Ontario Institute for Cancer Research (OICR)**, it exhibits over 40-fold selectivity against other histone methyltransferases and non-epigenetic targets. In cells, SGC3027 is converted to the active SGC8158 by reductases, inhibiting PRMT7-mediated arginine monomethylation of **HSP70** family proteins (e.g., at R469 on HSPA8), which reduces cellular tolerance to proteostatic stresses like heat shock and proteasome inhibition. It has shown potential in preclinical studies to enhance radiotherapy efficacy in non-small cell lung cancer (**NSCLC**) by suppressing tumor cell proliferation, migration, and invasion, though it has been withdrawn from commercial sale for research purposes.[1][3][5][8][10]

Other names

SGC3027N (negative control)