BrBzGCp2 (C09-1113-671)

BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC 50 of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activityIn VivoGLO1 inhibition by BrBzGCp2 increases center time in the OF test, without changing distance traveled. GLO1 inhibition increases MG (methylglyoxal) concentration, thus reducing anxiety-like behavior. BrBzGCp2 pre-treatment decreases seizure duration. BrBzGCp2 injection alleviates the level of anxiety in mice, and mice with less anxiety and fear were more likely to explore the unknown area, implying that inhibition of GLO1 activity mitigated anxiety levels. BrBzGCp2 treatment restores the VPA-induced inhibition effect on GABA A receptor activation. BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD-1 mice. Dosage: 50 mg/kg. Administration: IP once (Two hours post-injection, mice were sacrificed, and brains were rapidly dissected and flash-frozen on dry ice. MG concentration was measured) Result: Allowed MG levels to accumulate for 2 hoursForm:SolidIC50& Target:GC50: 4.23 μM (GLO1). Specification: 0.98 Molecular Formula: C27H38BrN3O6S Molecular Weight: 612.58 PubChem CID: 127939 Isomeric SMILES: C1CCC(C1)OC(=O)CNC(=O)[C@H](CSCC2=CC=C(C=C2)Br)NC(=O)CC[C@@H](C(=O)OC3CCCC3)N