GCN2iB | GCN2 inhibitor

GCN2iB chemical structure

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GCN2iB (2183470-12-2) is a potent (IC50 = 2.4 nM) and highly selective (against 468 kinases) inhibitor of general control nonderepressible 2 (GCN2), an important kinase involved in amino acid homeostasis. It displayed robust antitumor activity in xenografts of ALL, AML, and pancreatic cancers in conjunction with asparaginase treatment.1 GCN2iB alleviated adipocyte-mediated translation reducing their cytoprotective effect.2 It exhibited protective effects in mouse models of cerebral ischemia.3 GCN2iB alleviated hepatic steatosis in obese mice4 and hyperglycemia and insulin resistance in diabetic mice5. It also protected against cardiac dysfunction in diabetic mice.6

References/Citations:

  1. Nakamura et al. (2018), Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response; Proc. Natl. Acad. Sci. USA 115 E7776
  2. Heydt et al. (2021), Adipocytes disrupt the translational programme of acute lymphoblastic leukaemia to favour tumour survival and persistence; Nat. Commun. 12 5507
  3. Shi et al. (2019), GCN2 suppression attenuates cerebral ischemia in mice by reducing apoptosis and endoplasmic reticulum (ER) stress through the blockage of FoxO3a-regulated ROS production; Biochem. Biophys. Res. Commun.516 285
  4. Yuan et al. (2022), Inhibition of GCN2 alleviates hepatic steatosis and oxidative stress in obese mice: Involvement of NRF2 regulation; Redox Biol. 49 102224
  5. Yuan et al. (2022), Genetic and pharmacological inhibition of GCN2 Ameliorates Hyperglycemia and Insulin Resistance in Type 2 Diabetic Mice; Antioxidants (Basel) 11 1584
  6. Yuan et al. (2022), Inhibition of GCN2 Alleviates Cardiomyopathy in Type 2 Diabetic Mice via Attenuating Lipotoxicity and Oxidative Stress; Antioxidants (Basel) 11 1379
2183470-12-2, GCN2 inhibitor, GCN2iB, GCN2iB supplier

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GCN2iB (2183470-12-2) is a potent (IC50 = 2.4 nM) and highly selective (against 468 kinases) inhibitor of general control nonderepressible 2 (GCN2), an important kinase involved in amino acid homeostasis. It displayed robust antitumor activity in xenografts of ALL, AML, and pancreatic cancers in conjunction with asparaginase treatment.1 GCN2iB alleviated adipocyte-mediated translation reducing their cytoprotective effect.2 It exhibited protective effects in mouse models of cerebral ischemia.3 GCN2iB alleviated hepatic steatosis in obese mice4 and hyperglycemia and insulin resistance in diabetic mice5. It also protected against cardiac dysfunction in diabetic mice.6

References/Citations:

  1. Nakamura et al. (2018), Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response; Proc. Natl. Acad. Sci. USA 115 E7776
  2. Heydt et al. (2021), Adipocytes disrupt the translational programme of acute lymphoblastic leukaemia to favour tumour survival and persistence; Nat. Commun. 12 5507
  3. Shi et al. (2019), GCN2 suppression attenuates cerebral ischemia in mice by reducing apoptosis and endoplasmic reticulum (ER) stress through the blockage of FoxO3a-regulated ROS production; Biochem. Biophys. Res. Commun.516 285
  4. Yuan et al. (2022), Inhibition of GCN2 alleviates hepatic steatosis and oxidative stress in obese mice: Involvement of NRF2 regulation; Redox Biol. 49 102224
  5. Yuan et al. (2022), Genetic and pharmacological inhibition of GCN2 Ameliorates Hyperglycemia and Insulin Resistance in Type 2 Diabetic Mice; Antioxidants (Basel) 11 1584
  6. Yuan et al. (2022), Inhibition of GCN2 Alleviates Cardiomyopathy in Type 2 Diabetic Mice via Attenuating Lipotoxicity and Oxidative Stress; Antioxidants (Basel) 11 1379