179461-52-0

179461-52-0 structure

Name: PD 151746
Chemical Name: 2-Propenoic acid, 3-(5-fluoro-1H-indol-3-yl)-2-mercapto-
CAS Number: 179461-52-0
Molecular Formula: C₁₁H₈FNO₂S
Molecular Weight: 237.25000
Catalog: Biochemical Inhibitor Proteases Cysteine Protease Inhibitor
Create Date: 2018-11-23 20:40:42
Modify Date: 2024-01-01 19:01:30
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]

Name	2-Propenoic acid, 3-(5-fluoro-1H-indol-3-yl)-2-mercapto-
Synonyms	PD 151746 3-(5-Fluoro-1H-indol-3-yl)-2-mercapto-2-propenoic acid

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	Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome Research Areas >> Cardiovascular Disease
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.

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	powder,light orange to dark orange
Storage condition	-20°C
Water Solubility	Very slightly soluble (0.28 g/L) (25 ºC)

Safety Phrases	24/25
RIDADR	3077
WGK Germany	3

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