181765-30-0
Chemical Structure
PD 151746
- CAS No.: 181765-30-0
- Formula:C11H8FNO2S
- Molecular Weight:237.25
IUPAC Name: (Z)-3-(5-fluoro-1H-indol-3-yl)-2-mercaptoacrylic acid
InChIKey: HWMQHECFXSVZGN-KMKOMSMNSA-N
SMILES: O=C(O)/C(S)=C/C1=CNC2=C1C=C(F)C=C2
Biological Activity: PD 151746 is a selective calpain-1 inhibitor with an IC50 of 260 nM. PD 151746 binds μ-calpain Ca2+-binding sites, and shows selectivity over cathepsin B, papain, trypsin, thermolysin, and basal calcineurin. PD 151746 reduces Oxidized low-density lipoprotein (oxLDL)-induced cytotoxicity, apoptotic DNA fragmentation, and blocks IL-1α maturation. PD 151746 can be used for the research of atherosclerosis and psoriasis[1][2][3].
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PD 151746 | 95.0% | PD 151746 is a selective calpain-1 inhibitor with an IC50 of 260 nM. PD 151746 binds μ-calpain Ca2+-binding sites, and shows selectivity over cathepsin B, papain, trypsin, thermolysin, and basal calcineurin. PD 151746 reduces Oxidized low-density lipoprotein (oxLDL)-induced cytotoxicity, apoptotic DNA fragmentation, and blocks IL-1α maturation. PD 151746 can be used for the research of atherosclerosis and psoriasis. | ||||||||||||||||||||
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References
- [1]. Wang KK, et al. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. Proc Natl Acad Sci U S A. 1996;93(13):6687-6692. [Content Brief]
- [2]. Pörn-Ares MI, et al. Oxidized low-density lipoprotein induces calpain-dependent cell death and ubiquitination of caspase 3 in HMEC-1 endothelial cells. Biochem J. 2003 Sep 1;374(Pt 2):403-11. [Content Brief]
- [3]. Lei H, et al. Human S100A7 Induces Mature Interleukin1α Expression by RAGE-p38 MAPK-Calpain1 Pathway in Psoriasis. PLoS One. 2017;12(1):e0169788. Published 2017 Jan 6. [Content Brief]
