Glutaminase

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  1. transglutaminase 2 (TG2) inhibitor

    ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, which can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD).
  2. Glutaminase inhibitor

    CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.

  3. BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM.
  4. Glutamine antagonist

    HU-083 is a HU-083 is a Glutamine antagonist, a DON prodrug., a DON prodrug.
  5. KGA inhibitor

    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM.
  6. GAC inhibitor

    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  7. transglutaminase 2 (TGase) inhibitor

    GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
  8. 6-Diazo-5-oxo-L-nor-Leucine is a glutamine antagonist that shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 

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