SAL-003 | CAS# 1164470-53-4 | eIF2α dephosphorylation inhibitor

MedKoo Cat#: 530967 | Name: SAL003

Description:

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

SAL003 is a cell-permeable inhibitor of eIF2α dephosphorylation. SAL003 is an Analog of salubrinal with improved aqueous solubility. SAL003‑mediated upregulation of eIF2α phosphorylation suppressed cisplatin‑induced p53 activation. Furthermore, reduction of eIF2α phosphorylation by PERK knockdown enhanced cisplatin-induced p53 activation and apoptosis.

Chemical Structure

SAL003

CAS# 1164470-53-4

Theoretical Analysis

MedKoo Cat#: 530967

Name: SAL003

CAS#: 1164470-53-4

Chemical Formula: C18H15Cl4N3OS

Exact Mass: 460.9690

Molecular Weight: 463.20

Elemental Analysis: C, 46.68; H, 3.26; Cl, 30.61; N, 9.07; O, 3.45; S, 6.92

Price and Availability

Size	Price	Availability
1mg	USD 400.00	2 Weeks
10mg	USD 600.00	2 Weeks
50mg	USD 1,250.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

SAL-003; SAL 003; SAL003.

IUPAC/Chemical Name

3--Phenyl-N-(2,2,2-trichloro-1-((((4-chlorophenyl)amino)carbonothioyl)amino)ethyl)acrylamide

InChi Key

TVNBASWNLOIQML-IZZDOVSWSA-N

InChi Code

InChI=1S/C18H15Cl4N3OS/c19-13-7-9-14(10-8-13)23-17(27)25-16(18(20,21)22)24-15(26)11-6-12-4-2-1-3-5-12/h1-11,16H,(H,24,26)(H2,23,25,27)/b11-6+

SMILES Code

O=C(NC(NC(NC1=CC=C(Cl)C=C1)=S)C(Cl)(Cl)Cl)/C=C/C2=CC=CC=C2

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

To be determined

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

Cisplatin is one of the most widely used chemotherapeutic agents for the treatment of human cancers. However, the nephrotoxicity of cisplatin limits its use as a therapeutic agent. It has been suggested that oxidative stress and p53 activation play important roles in cisplatin-induced nephrotoxicity. It has been demonstrated that the eukaryotic translation initiation factor 2α (eIF2α) may protect HK-2 human renal proximal tubular cells against cisplatin-induced apoptosis through inhibition of reactive oxygen species (ROS)‑mediated p53 activation.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Sakuranetin is a cherry flavonoid phytoalexin that shows strong antifungal activity. Sakuranetin has anti-inflammatory and antioxidative activities. Sakuranetin ameliorates LPS-induced acute lung injury.

In vitro activity:

In HeLa cells, knockdown of eIF2α by siRNA or inhibition of eIF2α dephosphorylation by SAL003 enhanced SubAB-induced caspase activation. Reference: Infect Immun. 2012 May;80(5):1803-14. https://pubmed.ncbi.nlm.nih.gov/22354021/

In vivo activity:

Only early-long-term potentiationis evoked by repeated tetanic stimulation and long term memory is impaired when eIF2α phosphorylation is increased by injecting SAL003 into the hippocampus, which prevents the dephosphorylation of eIF2α. Reference: Cell. 2007 Apr 6;129(1):195-206. https://pubmed.ncbi.nlm.nih.gov/17418795/

Preparing Stock Solutions

The following data is based on the product molecular weight 463.20 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.

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. Soiberman US, Shehata AEM, Lu MX, Young T, Daoud YJ, Chakravarti S, Jun AS, Foster JW. Small Molecule Modulation of the Integrated Stress Response Governs the Keratoconic Phenotype In Vitro. Invest Ophthalmol Vis Sci. 2019 Aug 1;60(10):3422-3431. doi: 10.1167/iovs.19-27151. PMID: 31390655; PMCID: PMC6686743. 2. Yahiro K, Tsutsuki H, Ogura K, Nagasawa S, Moss J, Noda M. Regulation of subtilase cytotoxin-induced cell death by an RNA-dependent protein kinase-like endoplasmic reticulum kinase-dependent proteasome pathway in HeLa cells. Infect Immun. 2012 May;80(5):1803-14. doi: 10.1128/IAI.06164-11. Epub 2012 Feb 21. PMID: 22354021; PMCID: PMC3347452. 3. Peterson C, Kim YC, Ensign LM, Jun AS, Foster J. Induction of the integrated stress response in the rat cornea. Exp Eye Res. 2021 Sep;210:108722. doi: 10.1016/j.exer.2021.108722. Epub 2021 Aug 8. PMID: 34370978; PMCID: PMC8429264. 4. Costa-Mattioli M, Gobert D, Stern E, Gamache K, Colina R, Cuello C, Sossin W, Kaufman R, Pelletier J, Rosenblum K, Krnjević K, Lacaille JC, Nader K, Sonenberg N. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206. doi: 10.1016/j.cell.2007.01.050. PMID: 17418795; PMCID: PMC4149214.

In vitro protocol:

In vivo protocol:

1. Peterson C, Kim YC, Ensign LM, Jun AS, Foster J. Induction of the integrated stress response in the rat cornea. Exp Eye Res. 2021 Sep;210:108722. doi: 10.1016/j.exer.2021.108722. Epub 2021 Aug 8. PMID: 34370978; PMCID: PMC8429264. 2. Costa-Mattioli M, Gobert D, Stern E, Gamache K, Colina R, Cuello C, Sossin W, Kaufman R, Pelletier J, Rosenblum K, Krnjević K, Lacaille JC, Nader K, Sonenberg N. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206. doi: 10.1016/j.cell.2007.01.050. PMID: 17418795; PMCID: PMC4149214.

1: Mashayekhi-Sardoo H, Rezaee R, Yarmohammadi F, Karimi G. Targeting Endoplasmic Reticulum Stress by Natural and Chemical Compounds Ameliorates Cisplatin-Induced Nephrotoxicity: A Review. Biol Trace Elem Res. 2024 Aug 30. doi: 10.1007/s12011-024-04351-w. Epub ahead of print. PMID: 39212819. 2: Peng J, Huang J, Tan H, Kuang Y, Yang G, Huang Z. Model-Informed Dose Selection for a Novel Human Immunoglobulin G4 Derived Monoclonal Antibody Targeting Proprotein Convertase Kwashiorkor Type 9: Insights from Population Pharmacokinetics-Pharmacodynamics and Systems Pharmacology. ACS Pharmacol Transl Sci. 2024 Jan 17;7(2):406-420. doi: 10.1021/acsptsci.3c00256. PMID: 38357287; PMCID: PMC10863431. 3: Chen Y, Li B, Xu Y, Zhou T, Zhao C, Zhao J. Sal003 alleviated intervertebral disc degeneration by inhibiting apoptosis and extracellular matrix degradation through suppressing endoplasmic reticulum stress pathway in rats. Front Pharmacol. 2023 Jan 20;14:1095307. doi: 10.3389/fphar.2023.1095307. PMID: 36744257; PMCID: PMC9894885. 4: Chu HS, Peterson C, Chamling X, Berlinicke C, Zack D, Jun AS, Foster J. Integrated Stress Response Regulation of Corneal Epithelial Cell Motility and Cytokine Production. Invest Ophthalmol Vis Sci. 2022 Jul 8;63(8):1. doi: 10.1167/iovs.63.8.1. PMID: 35802384; PMCID: PMC9279922. 5: Peterson C, Kim YC, Ensign LM, Jun AS, Foster J. Induction of the integrated stress response in the rat cornea. Exp Eye Res. 2021 Sep;210:108722. doi: 10.1016/j.exer.2021.108722. Epub 2021 Aug 8. PMID: 34370978; PMCID: PMC8429264. 6: Fujita R, Jamet S, Lean G, Cheng HCM, Hébert S, Kleinman CL, Crist C. Satellite cell expansion is mediated by P-eIF2α-dependent Tacc3 translation. Development. 2021 Jan 20;148(2):dev194480. doi: 10.1242/dev.194480. PMID: 33318147. 7: Soiberman US, Shehata AEM, Lu MX, Young T, Daoud YJ, Chakravarti S, Jun AS, Foster JW. Small Molecule Modulation of the Integrated Stress Response Governs the Keratoconic Phenotype In Vitro. Invest Ophthalmol Vis Sci. 2019 Aug 1;60(10):3422-3431. doi: 10.1167/iovs.19-27151. PMID: 31390655; PMCID: PMC6686743. 8: Darini C, Ghaddar N, Chabot C, Assaker G, Sabri S, Wang S, Krishnamoorthy J, Buchanan M, Aguilar-Mahecha A, Abdulkarim B, Deschenes J, Torres J, Ursini- Siegel J, Basik M, Koromilas AE. An integrated stress response via PKR suppresses HER2+ cancers and improves trastuzumab therapy. Nat Commun. 2019 May 13;10(1):2139. doi: 10.1038/s41467-019-10138-8. PMID: 31086176; PMCID: PMC6513990. 9: Dadey DYA, Kapoor V, Khudanyan A, Thotala D, Hallahan DE. PERK Regulates Glioblastoma Sensitivity to ER Stress Although Promoting Radiation Resistance. Mol Cancer Res. 2018 Oct;16(10):1447-1453. doi: 10.1158/1541-7786.MCR-18-0224. Epub 2018 Jul 10. PMID: 29991528. 10: Werner CT, Stefanik MT, Milovanovic M, Caccamise A, Wolf ME. Protein Translation in the Nucleus Accumbens Is Dysregulated during Cocaine Withdrawal and Required for Expression of Incubation of Cocaine Craving. J Neurosci. 2018 Mar 14;38(11):2683-2697. doi: 10.1523/JNEUROSCI.2412-17.2018. Epub 2018 Feb 5. PMID: 29431650; PMCID: PMC5852654. 11: Ju SM, Jo YS, Jeon YM, Pae HO, Kang DG, Lee HS, Bae JS, Jeon BH. Phosphorylation of eIF2α suppresses cisplatin-induced p53 activation and apoptosis by attenuating oxidative stress via ATF4-mediated HO-1 expression in human renal proximal tubular cells. Int J Mol Med. 2017 Dec;40(6):1957-1964. doi: 10.3892/ijmm.2017.3181. Epub 2017 Oct 10. PMID: 29039478. 12: Jian M, Luo YX, Xue YX, Han Y, Shi HS, Liu JF, Yan W, Wu P, Meng SQ, Deng JH, Shen HW, Shi J, Lu L. eIF2α dephosphorylation in basolateral amygdala mediates reconsolidation of drug memory. J Neurosci. 2014 Jul 23;34(30):10010-21. doi: 10.1523/JNEUROSCI.0934-14.2014. PMID: 25057203; PMCID: PMC6608301. 13: Yahiro K, Tsutsuki H, Ogura K, Nagasawa S, Moss J, Noda M. Regulation of subtilase cytotoxin-induced cell death by an RNA-dependent protein kinase-like endoplasmic reticulum kinase-dependent proteasome pathway in HeLa cells. Infect Immun. 2012 May;80(5):1803-14. doi: 10.1128/IAI.06164-11. Epub 2012 Feb 21. PMID: 22354021; PMCID: PMC3347452. 14: Costa-Mattioli M, Gobert D, Stern E, Gamache K, Colina R, Cuello C, Sossin W, Kaufman R, Pelletier J, Rosenblum K, Krnjević K, Lacaille JC, Nader K, Sonenberg N. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206. doi: 10.1016/j.cell.2007.01.050. PMID: 17418795; PMCID: PMC4149214.