[CAS NO. 313649-08-0] Ucf-101
PRODUCTS SPECIFICATIONS [313649-08-0]
DESCRIPTION [313649-08-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 495.51 |
| Molecular Formula | C27H17N3O5S |
| SMILES | O=C(/C(C(N1C2=CC=CC=C2)=O)=C/C3=CC=C(C4=C([N+]([O-])=O)C=CC=C4)O3)N(C5=CC=CC=C5)C1=S |
Summary
Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2 , with an IC 50 of 9.5 μM for His-Omi . Ucf-101 exhibits very little activity against various other serine proteases (IC 50 >200 μM). 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 [1] [2] [3] .
IC50 & Target
IC50: 9.5 μM (His-Omi) [1]
In Vitro
Ucf-101 (20-100 μM; 30 min) inhibits the proteolytic activity of MBP-Omi-(134-458)
[1]
.
Ucf-101 (10-100 μM; pretreated for 10 min) inhibits His-Omi-(134-458) activity in a concentration-dependent manner when assayed with His-Omi-(134-458) and β-casein
[1]
.
Ucf-101 (1-25 μM; 36 h) inhibits Omi-induced caspase-independent apoptosis of mouse embryo caspase-9 (-/-) null fibroblasts
[1]
.
Ucf-101 (1-20 μM; pretreated for 1 h) inhibits the 6-OHDA-induced apoptosis of Parkinson’s disease (PD)-PC12 cells at the low concentration (2.5 μM), and increases the apoptosis rate at the high concentration (≥10 μM)
[3]
.
Ucf-101 (2.5 μM; pretreated for 1 h) downregulates the expression of Glucose-regulated protein 78 (Bip/Grp78) and C/EBP homologous protein (CHOP) in PD- PC12 cells
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ucf-101 (0.6-1.8 μmol/kg; a single i.p.) reduces postischemic myocardial apoptosis and myocardial infarct size in mice
[2]
.
Ucf-101 (1.5 μmol/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
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Adult male mice (20-25 g) with myocardial ischemia/reperfusion (MI/R) injury [1] |
| Dosage: | 0.6, 1.5, 1.8 μmol/kg |
| Administration: | I.p. 10 minutes before reperfusion |
| Result: | Reduced terminal dUTP nick end-labeling staining, incidence of DNA ladder fragmentation, and infarct size. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 12.5 mg/mL ( 25.23 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0181 mL | 10.0906 mL | 20.1812 mL |
| 5 mM | 0.4036 mL | 2.0181 mL | 4.0362 mL |
| 10 mM | 0.2018 mL | 1.0091 mL | 2.0181 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 1.79 mg/mL (3.61 mM); Suspended solution; Need ultrasonic
-
2.
References
- [1] Cilenti L, et, al. Characterization of a novel and specific inhibitor for the pro-apoptotic protease Omi/HtrA2. J Biol Chem. 2003 Mar 28;278(13):11489-94.
- [2] Liu HR, et, al. Role of Omi/HtrA2 in apoptotic cell death after myocardial ischemia and reperfusion. Circulation. 2005 Jan 4;111(1):90-6.
- [3] Li Y, et, al. Ucf-101 protects in vivoandin vitro models of PD against 6-hydroxydopamine toxicity by alleviating endoplasmic reticulum stress via the Wnt/β-catenin pathway. J Clin Neurosci. 2020 Jan;71:217-225.