PD 151746

Modify Date: 2024-01-01 19:01:30

PD 151746 Structure
PD 151746 structure
Common Name PD 151746
CAS Number 179461-52-0 Molecular Weight 237.25000
Density 1.525±0.06 g/cm3 Boiling Point N/A
Molecular Formula C11H8FNO2S Melting Point N/A
MSDS USA Flash Point N/A

 Use of PD 151746


PD151746 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]

 Names

Name 2-​Propenoic acid, 3-​(5-​fluoro-​1H-​indol-​3-​yl)​-​2-​mercapto-
Synonym More Synonyms

 PD 151746 Biological Activity

Description PD151746 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 Catalog
Cell Assay HMEC-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

Density 1.525±0.06 g/cm3
Molecular Formula C11H8FNO2S
Molecular Weight 237.25000
Exact Mass 237.02600
PSA 91.89000
LogP 2.66230
Appearance of Characters powder,light orange to dark orange
Storage condition -20°C
Water Solubility Very slightly soluble (0.28 g/L) (25 ºC)

 Safety Information

Safety Phrases 24/25
RIDADR 3077
WGK Germany 3

 Synonyms

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