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MedKoo Cat#: 531245 | Name: PD 150606
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PD 150606 is calpain inhibitor. PD150606 protects against ischemia/reperfusion injury by preventing μ-calpain-induced mitochondrial apoptosis. PD150606 attenuates glutamate induced spiral ganglion neuron apoptosis through apoptosis inducing factor pathway in vitro. PD150606) inhibits selective motor neuron death via inhibition of kainate-induced Ca2+ influx and not via calpain inhibition.

Chemical Structure

PD 150606
PD 150606
CAS#179528-45-1

Theoretical Analysis

MedKoo Cat#: 531245

Name: PD 150606

CAS#: 179528-45-1

Chemical Formula: C9H7IO2S

Exact Mass: 305.9211

Molecular Weight: 306.12

Elemental Analysis: C, 35.31; H, 2.30; I, 41.46; O, 10.45; S, 10.47

Price and Availability

Size Price Availability Quantity
200mg USD 950.00 2 Weeks
500mg USD 1,850.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 3,950.00 2 Weeks
5g USD 6,450.00 2 Weeks
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Related CAS #
No Data
Synonym
PD 150606; PD-150606; PD150606.
IUPAC/Chemical Name
3-(4-iodophenyl)-2Z-mercapto-2-propenoic acid
InChi Key
DJCVSFWGKYHMKH-YVMONPNESA-N
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-
SMILES Code
O=C(O)/C(S)=C/C1=CC=C(I)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor with Ki values of 0.21 μM and 0.37 μM.
In vitro activity:
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. Reference: Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92. https://pubmed.ncbi.nlm.nih.gov/8692879/
In vivo activity:
In a separate experiment, a pharmacological inhibitor of calpain PD150606 (Biomol, USA, 3 mg/kg/day, i.p.) daily for 30 days was given to mice after bleomycin injection on daily basis. Calpain activities increased in SSc-mouse lungs. Both deletion of Capns1 and administration of PD150606 attenuated dermal sclerosis as evidenced by a reduction of skin thickness and reduced interstitial fibrosis and inflammation in bleomycin model of SSc mice. Reference: Arthritis Res Ther. 2022 Jun 21;24(1):148. https://pubmed.ncbi.nlm.nih.gov/35729674/
Solvent mg/mL mM
Solubility
DMF 20.0 65.33
DMSO 26.2 85.60
DMSO:PBS (pH 7.2) (1:1) 0.5 1.63
Ethanol 8.7 28.27
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 306.12 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Luo T, Yue R, Hu H, Zhou Z, Yiu KH, Zhang S, Xu L, Li K, Yu Z. PD150606 protects against ischemia/reperfusion injury by preventing μ-calpain-induced mitochondrial apoptosis. Arch Biochem Biophys. 2015 Nov 15;586:1-9. doi: 10.1016/j.abb.2015.06.005. Epub 2015 Jun 16. PMID: 26091952. 2. Wang KK, Nath R, Posner A, Raser KJ, Buroker-Kilgore M, Hajimohammadreza I, Probert A W Jr, Marcoux FW, Ye Q, Takano E, Hatanaka M, Maki M, Caner H, Collins JL, Fergus A, Lee KS, Lunney EA, Hays SJ, Yuen P. 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. doi: 10.1073/pnas.93.13.6687. PMID: 8692879; PMCID: PMC39087. 3. Zhang L, Zheng D, Yan Y, Yu Y, Chen R, Li Z, Greer PA, Peng T, Wang Q. Myeloid cell-specific deletion of Capns1 prevents macrophage polarization toward the M1 phenotype and reduces interstitial lung disease in the bleomycin model of systemic sclerosis. Arthritis Res Ther. 2022 Jun 21;24(1):148. doi: 10.1186/s13075-022-02833-7. PMID: 35729674; PMCID: PMC9210712. 4. Yamaguchi T, Yoneyama M, Ogita K. Calpain inhibitor alleviates permanent hearing loss induced by intense noise by preventing disruption of gap junction-mediated intercellular communication in the cochlear spiral ligament. Eur J Pharmacol. 2017 May 15;803:187-194. doi: 10.1016/j.ejphar.2017.03.058. Epub 2017 Mar 31. PMID: 28366808.
In vitro protocol:
1. Luo T, Yue R, Hu H, Zhou Z, Yiu KH, Zhang S, Xu L, Li K, Yu Z. PD150606 protects against ischemia/reperfusion injury by preventing μ-calpain-induced mitochondrial apoptosis. Arch Biochem Biophys. 2015 Nov 15;586:1-9. doi: 10.1016/j.abb.2015.06.005. Epub 2015 Jun 16. PMID: 26091952. 2. Wang KK, Nath R, Posner A, Raser KJ, Buroker-Kilgore M, Hajimohammadreza I, Probert A W Jr, Marcoux FW, Ye Q, Takano E, Hatanaka M, Maki M, Caner H, Collins JL, Fergus A, Lee KS, Lunney EA, Hays SJ, Yuen P. 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. doi: 10.1073/pnas.93.13.6687. PMID: 8692879; PMCID: PMC39087.
In vivo protocol:
1. Zhang L, Zheng D, Yan Y, Yu Y, Chen R, Li Z, Greer PA, Peng T, Wang Q. Myeloid cell-specific deletion of Capns1 prevents macrophage polarization toward the M1 phenotype and reduces interstitial lung disease in the bleomycin model of systemic sclerosis. Arthritis Res Ther. 2022 Jun 21;24(1):148. doi: 10.1186/s13075-022-02833-7. PMID: 35729674; PMCID: PMC9210712. 2. Yamaguchi T, Yoneyama M, Ogita K. Calpain inhibitor alleviates permanent hearing loss induced by intense noise by preventing disruption of gap junction-mediated intercellular communication in the cochlear spiral ligament. Eur J Pharmacol. 2017 May 15;803:187-194. doi: 10.1016/j.ejphar.2017.03.058. Epub 2017 Mar 31. PMID: 28366808.
1: Metwally E, Al-Abbadi HA, Hashem MA, Mahmoud YK, Ahmed EA, Maaty AI, Helal IE, Ahmed MF. Selective Calpain Inhibition Improves Functional and Histopathological Outcomes in a Canine Spinal Cord Injury Model. Int J Mol Sci. 2022 Oct 4;23(19):11772. doi: 10.3390/ijms231911772. PMID: 36233068; PMCID: PMC9570220. 2: Melnikov IY, Tyganov SA, Sharlo KA, Ulanova AD, Vikhlyantsev IM, Mirzoev TM, Shenkman BS. Calpain-dependent degradation of cytoskeletal proteins as a key mechanism for a reduction in intrinsic passive stiffness of unloaded rat postural muscle. Pflugers Arch. 2022 Nov;474(11):1171-1183. doi: 10.1007/s00424-022-02740-5. Epub 2022 Aug 6. PMID: 35931829. 3: Shi H, Yu Y, Wang Y, Liu X, Yu Y, Li M, Zou Y, Chen R, Ge J. Inhibition of Calpain Alleviates Apoptosis in Coxsackievirus B3-induced Acute Virus Myocarditis Through Suppressing Endoplasmic Reticulum Stress. Int Heart J. 2021 Jul 30;62(4):900-909. doi: 10.1536/ihj.20-803. Epub 2021 Jul 6. PMID: 34234076. 4: Qian S, Li X, Wang H, Wei X, Mehmood W, Zhang C, Blecker C. Contribution of calpain to protein degradation, variation in myowater properties and the water- holding capacity of pork during postmortem ageing. Food Chem. 2020 Sep 15;324:126892. doi: 10.1016/j.foodchem.2020.126892. Epub 2020 Apr 21. PMID: 32339789. 5: Tomita T, Huibregtse JM, Matouschek A. A masked initiation region in retinoblastoma protein regulates its proteasomal degradation. Nat Commun. 2020 Apr 24;11(1):2019. doi: 10.1038/s41467-020-16003-3. PMID: 32332747; PMCID: PMC7181824. 6: Zou M, Zhang G, Zou J, Liu Y, Liu B, Hu X, Cheng Z. Inhibition of the ERK1/2-ubiquitous calpains pathway attenuates experimental pulmonary fibrosis in vivo and in vitro. Exp Cell Res. 2020 Jun 1;391(1):111886. doi: 10.1016/j.yexcr.2020.111886. Epub 2020 Feb 1. PMID: 32017927. 7: Lv Q, Yang J, Wang Y, Liu M, Feng Y, Wu G, Lin S, Yang Q, Hu J. Taurine Prevented Hypoxia Induced Chicken Cardiomyocyte Apoptosis Through the Inhibition of Mitochondrial Pathway Activated by Calpain-1. Adv Exp Med Biol. 2019;1155:451-462. doi: 10.1007/978-981-13-8023-5_42. PMID: 31468422. 8: Itoh R, Soejima T, Hiromatsu K. Anti-chlamydial activities of cell-permeable hydrophobic dipeptide-containing derivatives. J Infect Chemother. 2019 Dec;25(12):987-994. doi: 10.1016/j.jiac.2019.05.024. Epub 2019 Jun 20. PMID: 31230920. 9: Julien C, Tomberlin C, Roberts CM, Akram A, Stein GH, Silverman MA, Link CD. In vivo induction of membrane damage by β-amyloid peptide oligomers. Acta Neuropathol Commun. 2018 Nov 29;6(1):131. doi: 10.1186/s40478-018-0634-x. PMID: 30497524; PMCID: PMC6263551. 10: Petrova IO, Tyganov SA, Mirzoev TM, Tsaturyan AK, Kozlovskaya IB, Shenkman BS. Early Deсline in Rat Soleus Passive Tension with Hindlimb Unloading: Inactivation of Cross-bridges or Activation of Calpains? Dokl Biochem Biophys. 2018 Jul;481(1):205-207. doi: 10.1134/S1607672918040075. PMID: 30168060. 11: Chiarante N, García Vior MC, Rey O, Marino J, Roguin LP. Lysosomal permeabilization and endoplasmic reticulum stress mediate the apoptotic response induced after photoactivation of a lipophilic zinc(II) phthalocyanine. Int J Biochem Cell Biol. 2018 Oct;103:89-98. doi: 10.1016/j.biocel.2018.08.009. Epub 2018 Aug 18. PMID: 30130653. 12: Popik B, Crestani AP, Silva MO, Quillfeldt JA, de Oliveira Alvares L. Calpain modulates fear memory consolidation, retrieval and reconsolidation in the hippocampus. Neurobiol Learn Mem. 2018 May;151:53-58. doi: 10.1016/j.nlm.2018.04.002. Epub 2018 Apr 6. PMID: 29630999. 13: Baraban M, Koudelka S, Lyons DA. Ca 2+ activity signatures of myelin sheath formation and growth in vivo. Nat Neurosci. 2018 Jan;21(1):19-23. doi: 10.1038/s41593-017-0040-x. Epub 2017 Dec 11. PMID: 29230058; PMCID: PMC5742537. 14: Levin SG, Sirota NP, Nenov MN, Savina TA, Godukhin OV. Interleukin-10 and PD150606 modulate expression of AMPA receptor GluA1 and GluA2 subunits under hypoxic conditions. Neuroreport. 2018 Jan 17;29(2):84-91. doi: 10.1097/WNR.0000000000000928. PMID: 29112674. 15: Wang Q, Da'dara AA, Skelly PJ. The human blood parasite Schistosoma mansoni expresses extracellular tegumental calpains that cleave the blood clotting protein fibronectin. Sci Rep. 2017 Oct 10;7(1):12912. doi: 10.1038/s41598-017-13141-5. PMID: 29018227; PMCID: PMC5635006. 16: Rebai O, Belkhir M, Sanchez-Gomez MV, Matute C, Fattouch S, Amri M. Differential Molecular Targets for Neuroprotective Effect of Chlorogenic Acid and its Related Compounds Against Glutamate Induced Excitotoxicity and Oxidative Stress in Rat Cortical Neurons. Neurochem Res. 2017 Dec;42(12):3559-3572. doi: 10.1007/s11064-017-2403-9. Epub 2017 Sep 25. PMID: 28948515. 17: Tan WJ, Tan QY, Wang T, Lian M, Zhang L, Cheng ZS. Calpain 1 regulates TGF-β1-induced epithelial-mesenchymal transition in human lung epithelial cells via PI3K/Akt signaling pathway. Am J Transl Res. 2017 Mar 15;9(3):1402-1409. PMID: 28386365; PMCID: PMC5376030. 18: Yamaguchi T, Yoneyama M, Ogita K. Calpain inhibitor alleviates permanent hearing loss induced by intense noise by preventing disruption of gap junction- mediated intercellular communication in the cochlear spiral ligament. Eur J Pharmacol. 2017 May 15;803:187-194. doi: 10.1016/j.ejphar.2017.03.058. Epub 2017 Mar 31. PMID: 28366808. 19: Wang GJ, Wang Y, Teng YS, Sun FL, Xiang H, Liu JJ, Xia SL, Zhang GX, Chen HL, Shang D. Protective Effects of Emodin-Induced Neutrophil Apoptosis via the Ca2+-Caspase 12 Pathway against SIRS in Rats with Severe Acute Pancreatitis. Biomed Res Int. 2016;2016:1736024. doi: 10.1155/2016/1736024. Epub 2016 Dec 18. PMID: 28078280; PMCID: PMC5203873. 20: Wan F, Letavernier E, Abid S, Houssaini A, Czibik G, Marcos E, Rideau D, Parpaleix A, Lipskaia L, Amsellem V, Gellen B, Sawaki D, Derumeaux G, Dubois- Randé JL, Delcroix M, Quarck R, Baud L, Adnot S. Extracellular Calpain/Calpastatin Balance Is Involved in the Progression of Pulmonary Hypertension. Am J Respir Cell Mol Biol. 2016 Sep;55(3):337-51. doi: 10.1165/rcmb.2015-0257OC. PMID: 26974350.