Home Cart Sign in  
Chemical Structure| 1164470-53-4 Chemical Structure| 1164470-53-4

Structure of Sal003
CAS No.: 1164470-53-4

Chemical Structure| 1164470-53-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Sal003 is a potent cell-permeable analog of the eIF2α phosphatase inhibitor Salubrinal with enhanced aqueous solubility.

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Sal003

CAS No. :1164470-53-4
Formula : C18H15Cl4N3OS
M.W : 463.21
SMILES Code : O=C(NC(NC(NC1=CC=C(Cl)C=C1)=S)C(Cl)(Cl)Cl)/C=C/C2=CC=CC=C2
MDL No. :MFCD00361095
InChI Key :TVNBASWNLOIQML-IZZDOVSWSA-N
Pubchem ID :5717737

Safety of Sal003

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302+H312-H315-H318-H411
Precautionary Statements:P264-P270-P273-P280-P301+P312+P330-P302+P352+P312-P305+P351+P338+P310-P332+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse embryonic fibroblasts (MEFs) 10 μM 8 h Sal003 significantly increased eIF2α phosphorylation, inhibited general translation but selectively stimulated ATF4 mRNA translation PMC4149214
BM-132 cells 5 µM 14 days SAL003 significantly inhibited colony formation of patient-derived HER2+ breast cancer cells PMC6513990
BT474R cells 10 µM 3 h SAL003 activated the eIF2 α-P pathway in resistant cells and significantly potentiated the antiproliferative effects when combined with Trastuzumab PMC6513990
BT474S cells 10 µM 3 h SAL003 significantly increased eIF2 α-P, ATF4, P21CIP1 and JNK1/2 phosphorylation while decreasing DUSP1 expression, with enhanced effects when combined with Trastuzumab PMC6513990
corneal fibroblasts 2.5 µM 10 days In serum-containing media, SAL003 treatment resulted in decreased collagen production. PMC6686743
corneal fibroblasts 2.5 µM 3 days Activation of ISR resulted in increased eIF2α phosphorylation, ATF4 expression, CRP55 expression, and decreased collagen production. PMC6686743
rat nucleus pulposus cells 5 μM 24, 48, 72 h To evaluate the effects of Sal003 on cell viability and proliferation, results showed that 5 μM Sal003 significantly improved cell viability and inhibited apoptosis PMC9894885
NAc/PFC cocultured neurons 40 μM 2 h Validation of Sal003 efficacy in NAc MSNs using incorporation of the noncanonical amino acid AHA as a measure of new protein translation. Results showed that Sal003 significantly inhibited AHA incorporation in NAc MSN processes. PMC5852654

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Hippocampus-dependent fear conditioning model Bilateral hippocampal infusion 40 μM Single injection, lasting 30 minutes Sal003 injection prevented eIF2α dephosphorylation and significantly impaired long-term contextual fear memory PMC4149214
NOG mice HER2-positive gastric cancer PDX model Intratumoral injection 1.5 mg/kg Daily administration for 44 days SAL003 monotherapy partially inhibited tumor growth, while combination with Trastuzumab significantly enhanced antitumor effects and prolonged survival PMC6513990
Sprague-Dawley (SD) rats Needle puncture-induced intervertebral disc degeneration rat model Intradiscal injection 5 μM,5 μL Once a week for 4 weeks To evaluate the therapeutic effects of Sal003 on intervertebral disc degeneration, results showed that Sal003 significantly improved disc degeneration, reduced apoptosis and extracellular matrix degradation PMC9894885
Male Sprague Dawley rats Cocaine self-administration model Bilateral injection into the NAc core 20 μM, 0.5 μl Single injection 1 h or 15 min before the seeking test To test the effect of Sal003 on incubated cocaine seeking. Results showed that injection of Sal003 1 h or 15 min before the seeking test significantly reduced incubated cocaine seeking behavior. PMC5852654

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.59mL

4.32mL

2.16mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[1]Robert F, Kapp LD, et al. Initiation of protein synthesis by hepatitis C virus is refractory to reduced eIF2.GTP.Met-tRNA(i)(Met) ternary complex availability. Mol Biol Cell. 2006 Nov;17(11):4632-44. Epub 2006 Aug 23.

[2]Baltzis D, Pluquet O, et al. The eIF2alpha kinases PERK and PKR activate glycogen synthase kinase 3 to promote the proteasomal degradation of p53. J Biol Chem. 2007 Oct 26;282(43):31675-87. Epub 2007 Sep 4.

[3]Costa-Mattioli M, Gobert D, et al. eIF2alpha phosphorylation bidirectionally regulates the switch from short- to long-term synaptic plasticity and memory. Cell. 2007 Apr 6;129(1):195-206.

[4]Darini C, Ghaddar N, et al. An integrated stress response via PKR suppresses HER2+ cancers and improves trastuzumab therapy. Nat Commun. 2019 May 13;10(1):2139.

[5]Robert F, Kapp LD, Khan SN, Acker MG, Kolitz S, Kazemi S, Kaufman RJ, Merrick WC, Koromilas AE, Lorsch JR, Pelletier J. Initiation of protein synthesis by hepatitis C virus is refractory to reduced eIF2.GTP.Met-tRNA(i)(Met) ternary complex availability. Mol Biol Cell. 2006 Nov;17(11):4632-44. doi: 10.1091/mbc.e06-06-0478. Epub 2006 Aug 23. PMID: 16928960; PMCID: PMC1635388.

[6]Baltzis D, Pluquet O, Papadakis AI, Kazemi S, Qu LK, Koromilas AE. The eIF2alpha kinases PERK and PKR activate glycogen synthase kinase 3 to promote the proteasomal degradation of p53. J Biol Chem. 2007 Oct 26;282(43):31675-87. doi: 10.1074/jbc.M704491200. Epub 2007 Sep 4. PMID: 17785458.

[7]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.

 

Historical Records

Categories