UCF-101

Product NameUCF-101
CAS313649-08-0
MFC27H17N3O5S
MW495.51
EINECS
MOL FileMol File

Chemical Properties

Boiling point	651.8±65.0 °C(Predicted)
Density	1.50±0.1 g/cm3(Predicted)
storage temp.	-20°C
solubility	DMSO: soluble5mg/mL, clear (warmed)
pka	-0.92±0.20(Predicted)
form	powder
color	light orange to dark orange
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 1 month.
InChI	InChI=1S/C27H17N3O5S/c31-25-22(17-20-15-16-24(35-20)21-13-7-8-14-23(21)30(33)34)26(32)29(19-11-5-2-6-12-19)27(36)28(25)18-9-3-1-4-10-18/h1-17H
InChIKey	NVNSXBXKNMWKEJ-UHFFFAOYSA-N
SMILES	C1(=S)N(C2=CC=CC=C2)C(=O)/C(=C\C2=CC=C(C3=CC=CC=C3[N+]([O-])=O)O2)/C(=O)N1C1=CC=CC=C1

Safety Information

Hazard Codes	T
Risk Statements	25
Safety Statements	45
WGK Germany	3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

UCF-101 (313649-08-0) is a potent, specific, competitive, and reversible inhibitor of the pro-apoptotic, mitochondrial serine protease Omi/HtrA2 (IC50= 9.5 μM for His-Omi134-458). Shows very little activity against various other serine proteases tested (IC50≥ 200 μM).1Mitigates streptozotocin-induced cardiomyocyte dysfunction.2Protects against cerebral oxidative injury and cognitive impairment in a rat model.3 Cell permeable.

Uses

UCF 101 is a specific inhibitor of Omi/HtrA2, a proapoptotic mitochondrial serine protease. UCF 101 has the neuroprotective effects on cerebral oxidative injury and cognitive impairment in septic rats.

in vitro

ucf 101 was identified in a hts of a combinatorial library using omi-(134-458) protease and fluorescein-casein as a generic substrate. ucf 101 exhibited specific activity against omi/htra2 and very little activity against other serine proteases. ucf 101 showed a natural fluorescence that was used to monitor its ability to enter mammalian cells. in addition, when tested in caspase-9 (-/-) null fibroblasts, ucf 101 was able to inhibit omi/htra2-induced cell death [1].

in vivo

in a previous study, rats were intraperitoneally administered ucf-101 at 1.5 micromol/kg 10 min prior to reperfusion. results showed that ucf-101 treatment could significantly decrease cerebral infarct size by about 16.27% and also improve neurological behavior. moreover, ucf-101 treatment was able to reduce tunel-positive cells in the cerebral cortex significantly. in addition, the upregulation in the expression of fasl and the cleavage products of active caspase-3 and caspase-8 induced by ischemia was attenuated in mice treated with ucf-101, while upregulation of flip levels was increased [2].

IC 50

9.5 μm

References

[1] LUCIA CILENTI. Characterization of a novel and specific inhibitor for the pro-apoptotic protease Omi/HtrA2.[J]. The Journal of Biological Chemistry, 2003, 278 13: 11489-11494. DOI:10.1074/jbc.m212819200
[2] QUN LI Jun R Ji Li. UCF-101 mitigates streptozotocin-induced cardiomyocyte dysfunction: role of AMPK.[J]. American journal of physiology. Endocrinology and metabolism, 2009, 297 4: E965-73. DOI:10.1152/ajpendo.00323.2009
[3] YUEYU HU . Ucf-101 protects against cerebral oxidative injury and cognitive impairment in septic rat[J]. International immunopharmacology, 2013, 16 1: Pages 108-113. DOI:10.1016/j.intimp.2013.03.019

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