PD 150606

Non-peptide calpain inhibitor CAS# 179528-45-1

PD 150606

Catalog No. BCC2353----Order now to get a substantial discount!

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Chemical structure

PD 150606

3D structure

Chemical Properties of PD 150606

Cas No. 179528-45-1 SDF Download SDF
PubChem ID 9839500 Appearance Powder
Formula C9H7IO2S M.Wt 306.12
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 28 mg/mL (91.47 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name (Z)-3-(4-iodophenyl)-2-sulfanylprop-2-enoic acid
SMILES C1=CC(=CC=C1C=C(C(=O)O)S)I
Standard InChIKey DJCVSFWGKYHMKH-YVMONPNESA-N
Standard InChI InChI=1S/C9H7IO2S/c10-7-3-1-6(2-4-7)5-8(13)9(11)12/h1-5,13H,(H,11,12)/b8-5-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PD 150606

DescriptionSelective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively). Targets the calcium binding sites of calpain. Demonstrates high specificity for calpains relative to other proteases, and is a non-competitive inhibitor with respect to the substrate.

PD 150606 Dilution Calculator

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PD 150606 Molarity Calculator

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Preparing Stock Solutions of PD 150606

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2667 mL 16.3335 mL 32.6669 mL 65.3339 mL 81.6673 mL
5 mM 0.6533 mL 3.2667 mL 6.5334 mL 13.0668 mL 16.3335 mL
10 mM 0.3267 mL 1.6333 mL 3.2667 mL 6.5334 mL 8.1667 mL
50 mM 0.0653 mL 0.3267 mL 0.6533 mL 1.3067 mL 1.6333 mL
100 mM 0.0327 mL 0.1633 mL 0.3267 mL 0.6533 mL 0.8167 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on PD 150606

PD 150606 is a specific inhibitor of calpain with Ki value of 0.21 μM and 0.37 μM for mu- and m- calpains, respectively [1].
Calpain is an enzyme and plays an important role in a variety of physiological processes, including signaling, cytoskeletal remodeling, regulation of gene expression, apoptosis and cell cycle progression. It has been shown that calpain involves in many pathologies, like muscular dystrophies, cancer, diabetes, Alzheimer's disease and multiple sclerosis [2] [3].
PD 150606 is a potent calpain inhibitor and has similar activity as calpain inhibitor-III. When tested with A2058, A375 and HS578T cell lines infected with ΔPK(resulted the failure of cells growth in 3D culture), administration of PD 150606 in a concentration of 100 μM restored 3D growth in soft sugar culture by inhibiting calpain [2].
Treated pathogen-free adult C57BL/6 mice with PD 150606 (3 mg/kg, i.p) before LPS injection to establish sepsis mouse model that had lower myocardial calpain activity, the result showed that PD 150606 prevented the degradation of myocardial Hsp90/p-Akt protein induced by LPS and inhibited myocardial caspase-3 activation and apoptosis [3].
References:
[1].    Wang, K.K., 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): p. 6687-92.
[2].    Colunga, A., et al., Calpain-dependent clearance of the autophagy protein p62/SQSTM1 is a contributor to DeltaPK oncolytic activity in melanoma. Gene Ther, 2014. 21(4): p. 371-8.
[3].    Li, X., et al., The role of the Hsp90/Akt pathway in myocardial calpain-induced caspase-3 activation and apoptosis during sepsis. BMC Cardiovasc Disord, 2013. 13: p. 8.

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References on PD 150606

Sn- and Pd-Free Synthesis of D-pi-A Organic Sensitizers for Dye-Sensitized Solar Cells by Cu-Catalyzed Direct Arylation.[Pubmed:28371473]

ChemSusChem. 2017 May 22;10(10):2284-2290.

Predesigned Metal-Anchored Building Block for In Situ Generation of Pd Nanoparticles in Porous Covalent Organic Framework: Application in Heterogeneous Tandem Catalysis.[Pubmed:28368103]

ACS Appl Mater Interfaces. 2017 Apr 19;9(15):13785-13792.

The development of nanoparticle-polymer-hybrid-based heterogeneous catalysts with high reactivity and good recyclability is highly desired for their applications in the chemical and pharmaceutical industries. Herein, we have developed a novel synthetic strategy by choosing a predesigned metal-anchored building block for in situ generation of metal (Pd) nanoparticles in the stable, porous, and crystalline covalent organic framework (COF), without using conventional reducing agents. In situ generation of Pd nanoparticles in the COF skeleton is explicitly confirmed from PXRD, XPS, TEM images, and (15)N NMR spectral analysis. This hybrid material is found to be an excellent reusable heterogeneous catalyst for the synthesis of biologically and pharmaceutically important 2-substituted benzofurans from 2-bromophenols and terminal alkynes via a tandem process with the turnover number up to 1101. The heterogeneity of the catalytic process is unambiguously verified by a mercury poisoning experiment and leaching test. This hybrid material shows superior catalytic performance compared to commercially available homogeneous as well as heterogeneous Pd catalysts.

Tumor cell-intrinsic CD274/PD-L1: A novel metabolic balancing act with clinical potential.[Pubmed:28368722]

Autophagy. 2017 May 4;13(5):987-988.

Tumor expression of the immune co-signaling molecule CD274/PD-L1 was originally described as impeding antitumor immunity by direct engagement of its receptor, PDCD1/PD-1, on antitumor T cells. Melanoma-intrinsic PDCD1 was recently shown to promote tumor growth and MTOR signals in cooperation with tumor CD274, and sarcoma-intrinsic CD274 signaling promotes glucose metabolism to impede antitumor immunity. Our recent report shows that tumor cell-intrinsic CD274 promotes MTORC1 signaling in mouse melanoma and mouse and human ovarian cancer, inhibits autophagy and sensitizes some tumors to clinically available pharmacological autophagy inhibitors and confers resistance to MTOR inhibitors. Tumor CD274 could be a biomarker of autophagy or MTOR inhibitor response in selected tumors, and these inhibitors could improve anti-CD274 or anti-PDCD1 cancer immunotherapy. As we found that distinct tumor types exhibit this CD274-driven phenotype, it could be widely applicable.

Calpains mediate calcium and chloride influx during the late phase of cell injury.[Pubmed:9399991]

J Pharmacol Exp Ther. 1997 Dec;283(3):1177-84.

The role of Ca++ in cell death is controversial. Extracellular Ca++ influx and calpain activation occurred during the late phase of renal proximal tubule cell injury produced by the mitochondrial inhibitor antimycin A. Chelation of intracellular Ca++, extracellular Ca++, the calcium channel blocker nifedipine, calpain inhibitor 1 and the dissimilar calpain inhibitor PD150606 blocked antimycin A-induced influx of extracellular Ca++ and cell death. The calcium channel blocker verapamil was ineffective. Calpain inhibitor 1 and PD150606 were cytoprotective also against tetrafluoroethyl-L-cysteine-, bromohydroquinone-, oxidant (t-butylhydroperoxide)- and calcium ionophore (ionomycin)-induced cell death. Extracellular Ca++ influx was associated with the translocation of calpain activity from the cytosol to the membrane and was prevented by calpain inhibitor 1, PD150606 and nifedipine. Finally, nifedipine, calpain inhibitor 1, PD150606 and the Cl- channel inhibitors [5-nitro-2-(3-phenylpropylamino)-benzoate, niflumic acid, diphenylamine-2-carboxylate, and indanyloxyacetic acid] blocked the increase in Cl- influx that occurs during the late phase of cell injury and triggers terminal cell swelling and death. These data suggest that Ca++ and calpains play a common and critical role in renal proximal tubule cell death produced by diverse agents. In addition, calpain activation appears to play a dual role during the late phase of cell injury. Initial calpain activation elicits extracellular Ca++ influx through a nifedipine-sensitive pathway, resulting in calpain translocation to the membrane and in turn Cl- influx.

An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective.[Pubmed:8692879]

Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92.

Overactivation of calcium-activated neutral protease (calpain) has been implicated in the pathophysiology of several degenerative conditions, including stroke, myocardial ischemia, neuromuscular degeneration, and cataract formation. Alpha-mercaptoacrylate derivatives (exemplified by PD150606), with potent and selective inhibitory actions against calpain, have been identified. PD150606 exhibits the following characteristics: (i) Ki values for mu- and m-calpains of 0.21 microM and 0.37 microM, respectively, (ii) high specificity for calpains relative to other proteases, (iii) uncompetitive inhibition with respect to substrate, and (iv) it does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane, suggesting a nonactive site action for PD150606. The recombinant calcium-binding domain from each of the large or small subunits of mu-calpain was found to interact with PD150606. In low micromolar range, PD15O6O6 inhibited calpain activity in two intact cell systems. The neuroprotective effects of this class of compound were also demonstrated by the ability of PD150606 to attenuate hypoxic/hypoglycemic injury to cerebrocortical neurons in culture and excitotoxic injury to Purkinje cells in cerebellar slices.

Description

PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM for μ- and m-calpains respectively, which is neuroprotective.

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