PD 150606 |
Catalog No.GC16912
One-Click Copy Product Info
|
An inhibitor of calpains
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 179528-45-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
| Cas No. | 179528-45-1 | SDF | |
| Chemical Name | (Z)-3-(4-iodophenyl)-2-sulfanylprop-2-enoic acid | ||
| Canonical SMILES | C1=CC(=CC=C1C=C(C(=O)O)S)I | ||
| Formula | C9H7IO2S | M.Wt | 306.12 |
| Solubility | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 2 mg/ml | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2667 mL | 16.3335 mL | 32.6669 mL |
| 5 mM | 653.3 μL | 3.2667 mL | 6.5334 mL |
| 10 mM | 326.7 μL | 1.6333 mL | 3.2667 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)