Ucf-101

313649-08-0

495.51

H₂O : < 0.1 mg/mL; DMSO : 12.5 mg/mL (ultrasonic)

Apoptosis

Ucf-101 is a selctive and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 uM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 uM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.
IC50 & Target: IC50: 9.5 uM (His-Omi)
In Vitro: Ucf-101 (20-100 uM; 30 min) inhibits the proteolytic activity of MBP-Omi-(134-458).

Ucf-101 (10-100 uM; pretreated for 10 min) inhibits His-Omi-(134-458) activity in a concentration-dependent manner when assayed with His-Omi-(134-458) and beta-casein.

Ucf-101 (1-25 uM; 36 h) inhibits Omi-induced caspase-independent apoptosis of mouse embryo caspase-9 (-/-) null fibroblasts.

Ucf-101 (1-20 uM; pretreated for 1 h) inhibits the 6-OHDA-induced apoptosis of Parkinson's disease (PD)-PC12 cells at the low concentration (2.5 uM), and increases the apoptosis rate at the high concentration (>=10 uM).

Ucf-101 (2.5 uM; pretreated for 1 h) downregulates the expression of Glucose-regulated protein 78 (Bip/Grp78) and C/EBP homologous protein (CHOP) in PD- PC12 cells.
In Vivo: Ucf-101 (0.6-1.8 umol/kg; a single i.p.) reduces postischemic myocardial apoptosis and myocardial infarct size in mice.

Ucf-101 (1.5 umol/kg; a single i.p.) improves the APO-induced rotational behavior, increases the TH-positive cells and reverses the reduction of DA neurons in the PD rats.