| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PD 150606 targets calpain, a family of calcium-activated cysteine proteases that play a critical role in various physiological and pathological processes, including apoptosis, cell signaling, and neurodegeneration. The compound is a selective, cell-permeable, non-peptide, uncompetitive calpain inhibitor. It exhibits Ki values of 0.21 µM for μ-calpain and 0.37 µM for m-calpain.
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| ln Vitro |
The u- and m-calcium-binding domains are interacting with PD150606 [1]. The effects of cycloheximide (10 mg/mL) induction Granular cell disinfection are lessened by PD 150606 (25 μM; 0–12 hours), which also attenuates hypoxic/hypoglycemic harm to mesocortical neurons and caused toxic injury to Purkinje cells [2].
In vitro, PD 150606 inhibits calpain activity with Ki values of 0.21 µM (μ-calpain) and 0.37 µM (m-calpain). The compound (25 µM; 0-12 hours) reduces cycloheximide-induced neutrophil apoptosis to some extent. PD 150606 inhibits kainate-induced Ca²⁺ influx and interferes with excitotoxicity-dependent motor neuron death. |
| ln Vivo |
In vivo, PD 150606 has been evaluated in animal models of neurodegeneration and excitotoxicity. As a calpain inhibitor, it has demonstrated neuroprotective effects by reducing excitotoxic damage in cerebellar Purkinje cells. The compound's ability to inhibit calpain-mediated proteolysis supports its investigation for neuroprotective indications.
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| Enzyme Assay |
In vitro enzyme assays for calpain inhibition involve incubating purified μ-calpain or m-calpain with a fluorogenic peptide substrate and Ca²⁺ in the presence of varying concentrations of PD 150606. The cleavage of the substrate is measured fluorometrically, and Ki values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays are performed using neurons or other cell types expressing calpain. Cells are treated with PD 150606 at various concentrations and then subjected to apoptotic or excitotoxic stimuli. Calpain activity is assessed by measuring the cleavage of calpain substrates such as spectrin by Western blot. Cell viability and apoptosis are evaluated by MTT or flow cytometry.
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| Animal Protocol |
In vivo studies are conducted in rodent models of neurodegeneration, such as excitotoxicity or ischemia. PD 150606 is administered intraperitoneally or intracerebroventricularly at various doses. Neuroprotection is assessed by histological analysis of neuronal damage and by behavioral tests.
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| ADME/Pharmacokinetics |
PD 150606 (molecular weight 306.12, formula C₉H₇IO₂S) is a small-molecule compound. It is a cell-permeable, non-peptide calpain inhibitor. The compound is soluble in DMSO and is typically stored at -20°C. Its physicochemical properties support its use in both in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of PD 150606 have been limited, as the compound is primarily used as a research tool. No significant toxicity has been reported in the available literature. The compound's safety profile supports its use for studying calpain function.
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| References | |
| Additional Infomation |
(Z)-3-(4-iodophenyl)-2-mercaptoacrylic acid is an organoiodine compound, a derivative of acrylic acid, in which the vinyl hydrogens at positions 2 and 3 are replaced by thiol groups and 4-iodophenyl groups, respectively (Z-isomer). It exhibits inhibitory effects on calpain and apoptosis. It is an organoiodine compound belonging to the cinnamic acid and thioenol classes. Functionally, it is related to trans-cinnamic acid.
PD 150606 is a potent and selective non-peptide calpain inhibitor. Its mechanism involves uncompetitive inhibition of calpain, blocking calcium-dependent proteolysis. The compound has neuroprotective effects and has been used to study the role of calpain in apoptosis, neurodegeneration, and excitotoxicity. PD 150606 is primarily used for research purposes and has not received regulatory approval for clinical use. |
| Molecular Formula |
C9H7O2SI
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|---|---|
| Molecular Weight |
306.11968
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| Exact Mass |
305.921
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| CAS # |
179528-45-1
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| PubChem CID |
9839500
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
410.4±45.0 °C at 760 mmHg
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| Flash Point |
202.0±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.732
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| LogP |
4.25
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
220
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1/C=C(/C(=O)O)\S)I
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| InChi Key |
DJCVSFWGKYHMKH-YVMONPNESA-N
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| InChi Code |
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-
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| Chemical Name |
3-(4-iodophenyl)-2Z-mercapto-2-propenoic acid
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| Synonyms |
PD 150606; PD-150606; PD150606.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 28 mg/mL (~91.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.17 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2667 mL | 16.3335 mL | 32.6669 mL | |
| 5 mM | 0.6533 mL | 3.2667 mL | 6.5334 mL | |
| 10 mM | 0.3267 mL | 1.6333 mL | 3.2667 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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