Structure of Salermide
CAS No.: 1105698-15-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Salermide, a reverse amide, can act as an inhibitor of sirt, especially of sirt2, with the property of inducing apoptosis of tumor cells.
Synonyms: Salermide
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CAS No. : | 1105698-15-4 |
Formula : | C26H22N2O2 |
M.W : | 394.47 |
SMILES Code : | CC(C1=CC=CC=C1)C(NC2=CC=CC(/N=C/C3=C4C=CC=CC4=CC=C3O)=C2)=O |
Synonyms : |
Salermide
|
InChI Key : | HQSSEGBEYORUBY-UHFFFAOYSA-N |
Pubchem ID : | 135659046 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H317-H412 |
Precautionary Statements: | P273-P280 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Acanthamoeba castellanii trophozoites | 100 μM | 24 and 48 hours | Inhibited the proliferation of Acanthamoeba castellanii trophozoites | PMC7376869 |
H1650 | 20 μM | 24 hours | To evaluate the apoptosis effect of Salermide on H1650 cells, results showed H1650 cells were particularly sensitive to Salermide. | PMC3823229 |
HCT116 Oxa-R cells | 20 μM | 24 hours | To evaluate the effect of CAY10602 on oxaliplatin resistance, results showed that CAY10602 enhancement of SIRT1 expression decreased the resistance of HCT116 Oxa-R cells to oxaliplatin. | PMC11924001 |
HCT116 Oxa-R cells | 10 μM | 24 hours | To evaluate the effect of Salermide on oxaliplatin resistance, results showed that Salermide inhibition of SIRT1 expression increased the resistance of HCT116 Oxa-R cells to oxaliplatin. | PMC11924001 |
BxPC-3 cells | 5-100 µM | 24 hours | To evaluate the effect of Salermide alone or in combination with EF24 on the viability of BxPC-3 cells. Results showed that Salermide alone significantly reduced the viability of BxPC-3 cells with an IC50 value of approximately 40 µM. | PMC4908665 |
H157 | 50 μM | 24, 48 hours | To evaluate the time-dependent apoptosis induced by Salermide, results showed apoptosis started at 24 hrs and peaked at 48 hrs. | PMC3823229 |
Acanthamoeba castellanii trophozoites | 100 μM | 24, 48, 72 hours | Inhibited the proliferation of Acanthamoeba castellanii trophozoites | PMC7376869 |
Human brain microvascular endothelial cells and astrocytes co-culture model | 50 μM | 30 min pretreatment | Sirt1 inhibition significantly reduced BBB permeability (increased TEER) and attenuated OGD-induced apoptosis and mitochondrial ROS generation | PMC5633840 |
SKOV-3 cells | 50 μM | 48 hours | Comparison of anticancer effects between MHY2256 and salermide in SKOV-3 cells, showing IC50 values of salermide as 36.5-50.9 μM | PMC5166496 |
MCF-7 cells | 50 μM | 48 hours | Comparison of anticancer effects between MHY2256 and salermide in MCF-7 cells, showing IC50 values of salermide as 36.5-50.9 μM | PMC5166496 |
H1792 | 12.5, 25, 50 μM | 48 hours | To evaluate the effect of Salermide on cell growth, results showed Salermide induced growth inhibition in a concentration-dependent manner. | PMC3823229 |
Ishikawa endometrial cancer cells | 0.1–50 μM | 48 hours | To compare the cytotoxicity of MHY2256 and Salermide on Ishikawa cells. Results showed that the IC50 value of MHY2256 was approximately 10-fold lower than that of salermide. | PMC6164480 |
LLCMK2 cells | 2 μM | 48 hours | Salermide reduced the number of intracellular parasites in vitro infection assays with minimal effects on host cell viability. | PMC4505258 |
MiaPaca-2 pancreatic cancer cells | 25–50 μM | 72 hours | Inhibited SIRT2 activity, reduced c-Myc protein expression, and suppressed cell proliferation | PMC3569991 |
BE(2)-C neuroblastoma cells | 25–50 μM | 72 hours | Inhibited SIRT2 activity, reduced N-Myc protein expression, and suppressed cell proliferation | PMC3569991 |
Trypanosoma cruzi epimastigotes | 5 μM | 72 hours | Salermide significantly inhibited parasite growth and differentiation, with an EC50 of 10.6 μM. | PMC4505258 |
Acanthamoeba castellanii encysting cells | 100 μM | 72 hours | Inhibited the encystation of Acanthamoeba castellanii | PMC7376869 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Zebrafish | Dmd mutant zebrafish | Embryo bath | 1 μM | From 1 dpf to 4 dpf, changing the treatment solution daily | To evaluate the effect of Salermide in combination with oxamflatin on the skeletal muscle structure of dmd mutant zebrafish. Results showed that the combination significantly ameliorated skeletal muscle degeneration. | PMC7559456 |
BALB/c nude mice | Subcutaneous xenograft model of HCT116 Oxa-R cells in nude mice | Subcutaneous injection | 10 mg/kg | Three times a week until tumor volume reached 1500 mm³ | To evaluate the effect of CAY10602 on oxaliplatin resistance, results showed that CAY10602 enhanced the growth-inhibitory effect of oxaliplatin on HCT116 Oxa-R cells. | PMC11924001 |
BALB/c mice | Chagas disease model | Intraperitoneal injection | 100 μM | Daily for 12 days | Salermide partially controlled in vivo infection, reducing parasitemia. | PMC4505258 |
Nude mice | MCF-7 xenograft model | Intraperitoneal injection | 30 mg/kg | Once per week for 4 weeks | Evaluation of the antitumor effects of salermide in the MCF-7 xenograft model, showing significant inhibition of tumor growth | PMC5166496 |
Nude mice | Ishikawa endometrial cancer cell xenograft model | Intraperitoneal injection | 30 mg/kg | Once per week for 30 days | To evaluate the antitumor effect of Salermide on Ishikawa cell xenograft model. Results showed that salermide significantly inhibited tumor growth. | PMC6164480 |
Mice | Photothrombotic stroke model | Intracerebroventricular injection | 400 μM | Single administration, 1 hour after stroke | To study the effect of Salermide on infarction volume and apoptotic index after stroke. Results showed that Salermide did not significantly alter infarction volume or apoptotic index compared to control samples. | PMC9092253 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.54mL 0.51mL 0.25mL |
12.68mL 2.54mL 1.27mL |
25.35mL 5.07mL 2.54mL |
Tags: Salermide | Sirtuin | Apoptosis | Sirt1 Inhibitor | Sirt2 Inhibitor | sirtuin inhibition | 1105698-15-4
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