PD 151746

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PD 151746 is a potent and selective inhibitor of calpain with Ki value of 0.26 μM for μ-Calpain.
Calpain is a calcium-dependent, non-lysosomal cysteine protease that expressed in mammals and many other organisms. Calpain plays an important role in cell mobility and cell cycle progression.
PD 151746 is a cell-permeable, potent and selective calpain inhibitor. PD151746 significantly inhibited NMDA-induced α-spectrin breakdown product (SBDP) of 145 kDa and completely inhibited the fragmentation of calmodulin-dependent protein kinase II-α (CaMPK-IIα) and nitric oxide synthase (nNOS), which were cleaved by calpain [1]. In cerebellar granule cells, PD151746 inhibited serum/potassium (S/K) withdrawal induced apoptosis by 29% through inhibition of calpain. Also, PD151746 inhibited the increase of MEF2 phosphorylation and cdk5/p25 formation and inhibited caspase-3 activity [2]. In human hepatoma G2 cells, PD151746 significantly reduced insulin-stimulated glycogen synthesis and increased the amount of protein tyrosine phosphatase-ε (PTPε), which suggested that calpain played an important role in regulation of insulin-stimulated glycogen synthesis [3]. In HEK-293 cells expressing human formyl peptide receptor (hFPR) or hFPR-like 1 (hFPRL1), PD151746 increased cytoplasmic free Ca2+ ([Ca2+]i) [4].
References:
[1]. Hajimohammadreza I, Raser KJ, Nath R, et al. Neuronal nitric oxide synthase and calmodulin-dependent protein kinase IIalpha undergo neurotoxin-induced proteolysis. J Neurochem, 1997, 69(3): 1006-1013.
[2]. Verdaguer E, Alvira D, Jiménez A, et al. Inhibition of the cdk5/MEF2 pathway is involved in the antiapoptotic properties of calpain inhibitors in cerebellar neurons. Br J Pharmacol, 2005, 145(8): 1103-1011.
[3]. Meier M, Klein HH, Kramer J, et al. Calpain inhibition impairs glycogen syntheses in HepG2 hepatoma cells without altering insulin signaling. J Endocrinol, 2007, 193(1): 45-51.
[4]. Fujita H, Kato T, Watanabe N, et al. Stimulation of human formyl peptide receptors by calpain inhibitors: homology modeling of receptors and ligand docking simulation. Arch Biochem Biophys, 2011, 516(2): 121-127.
Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 237.25 |
Cas No. | 179461-52-0 |
Formula | C11H8FNO2S |
Solubility | insoluble in H2O; ≥11.6 mg/mL in DMSO; ≥12.78 mg/mL in EtOH |
Chemical Name | (Z)-3-(5-fluoro-1H-indol-3-yl)-2-mercaptoacrylic acid |
SDF | Download SDF |
Canonical SMILES | FC1=CC(C(/C([H])=C(S)/C(O)=O)=CN2)=C2C=C1 |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment [1]: | |
Cell lines |
Cerebellar granule cells |
Preparation method |
The solubility of this compound in DMSO is > 11.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition |
20 or 40 μM; 24 hrs |
Applications |
In cerebellar granule cells, pre-treatment with 20 or 40 μM PD 151746 for 24 hrs inhibited calpain and thus, protected neurons against the effect of serum/potassium (S/K) withdrawal, restoring the number of cell survival. Moreover, PD 151746 at the dose of 40 μM inhibited the increase of MEF2 phosphorylation and cdk5/p25 formation, as well as inhibited caspase-3 activity. |
References: [1]. Verdaguer E, Alvira D, Jiménez A, et al. Inhibition of the cdk5/MEF2 pathway is involved in the antiapoptotic properties of calpain inhibitors in cerebellar neurons. Br J Pharmacol, 2005, 145(8): 1103-1011. |
Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
