CAS 179461-52-0|PD 151746

Introduction:Basic information about CAS 179461-52-0|PD 151746, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NamePD 151746
CAS Number179461-52-0Molecular Weight237.25000
Density1.525±0.06 g/cm3Boiling Point/
Molecular FormulaC11H8FNO2SMelting Point/
MSDSUSAFlash Point/

Names

Name2-​Propenoic acid, 3-​(5-​fluoro-​1H-​indol-​3-​yl)​-​2-​mercapto-
SynonymMore Synonyms

PD 151746 BiologicalActivity

DescriptionPD151746 is a calpain inhibitor, shows a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM).IC50 value: 0.26 ± 0.03 μM (Ki, for μ-calpain), 5.33 ± 0.77 μM (Ki, for m-calpain) [1]Target: calpainin vitro: The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity. [2]
Related CatalogSignaling Pathways >>Metabolic Enzyme/Protease >>ProteasomeResearch Areas >>Cardiovascular Disease
Cell AssayHMEC-1 cells cultured in 60-mm-diameter culture dishes were left untreated or were exposed to 200 μg/ml oxLDL for 20 h or to 200 nM staurosporine (STS) for 4 h. Along with oxLDL, some cells were co-treated with PD 151746 (20 μM) or BAF (50 μM). Thereafter, the cells were harvested and processed for Western blotting as described in the Experimental section. The PVDF membrane was probed with an anti-α-fodrin mAb. The absorbance (A) of the 150 and 120 kDa bands was scanned, and the ratio of the two values (A 150/A 120) is indicated below relevant samples. The illustrated blot is representative of five separate experiments[2].
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 Jun 25;93(13):6687-92.

[2]. P?rn-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.

Chemical & Physical Properties

Density1.525±0.06 g/cm3
Molecular FormulaC11H8FNO2S
Molecular Weight237.25000
Exact Mass237.02600
PSA91.89000
LogP2.66230
Appearance of Characterspowder,light orange to dark orange
InChIKeyHWMQHECFXSVZGN-KMKOMSMNSA-N
SMILESO=C(O)C(S)=Cc1c[nH]c2ccc(F)cc12
Storage condition-20°C
Water SolubilityVery slightly soluble (0.28 g/L) (25 ºC)

Safety Information

Safety Phrases24/25
RIDADR3077
WGK Germany3

Synonyms

PD 151746
3-(5-Fluoro-1H-indol-3-yl)-2-mercapto-2-propenoic acid
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