TrxR1-IN-B19
TrxR1-IN-B19 (GO-Y015) is a Curcumin (HY-N0005) derivative and TrxR1 inhibitor. TrxR1-IN-B19 inhibits de novo selenoprotein synthesis, suppresses SeP and GPx expression, and impairs selenium incorporation into Sec-tRNA[Sec]. TrxR1-IN-B19 induces Nrf2 accumulation through Keap1 cysteine modification, HO-1 expression, GSH synthesis, ROS accumulation, ER stress, mitochondrial dysfunction, Apoptosis, and G2/M phase arrest. TrxR1-IN-B19 improves glucose tolerance and insulin sensitivity, lowers blood glucose, inhibits tumor growth, and reduces arsenic accumulation. TrxR1-IN-B19 can be used for research on type 2 diabetes, arsenite-induced toxicity, and gastric cancer.
For research use only. We do not sell to patients.
- CAS No.: 170950-29-5
- Formula: C21H22O5
- Molecular Weight:354.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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HO-1 |
TrxR1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SGC-7901 | IC50 |
13.9 μM
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Cytotoxicity against human SGC-7901 gastric cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human SGC-7901 gastric cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
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26919094 |
| BGC-823 | IC50 |
14.2 μM
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Cytotoxicity against human BGC-823 gastric cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human BGC-823 gastric cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
26919094 |
| KATO III stomach cancer cell line | IC50 |
13.1 μM
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Cytotoxicity against human KATO III gastric cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Cytotoxicity against human KATO III gastric cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
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26919094 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2
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Concentration:up to 8 μM
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Incubation Time:24 h
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Result:Showed minimal cytotoxicity up to 8 μM.
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Cell Line:HepG2
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Concentration:> 5 µM
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Incubation Time:6 h
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Result:Effectively protected against As(III) toxicity when pretreated at concentrations greater than 5 µM.
Increased the TD50 of As(III) to 261.5 µM.
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Cell Line:HepG2
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Concentration:2-8 µM
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Incubation Time:6 h
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Result:Resulted in Nrf2 accumulation and HO-1 protein expression increases in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 12 hours; 48 hours
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Result:Significantly decreased serum SeP protein levels.
Reduced hepatic GPx4 levels.
Did not alter mRNA expression of genes involved in selenium metabolism, SeP synthesis, and Nrf2 downstream pathways.
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Animal Model:KK-Ay (male, 10 weeks old)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; every 12 hours; 48 hours
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Result:At 10 mg/kg, failed to reduce SeP expression and failed to improve GTT.
At 30 mg/kg, decreased serum SeP levels while GPx levels remained unchanged.
After only two injections at 30 mg/kg, random blood glucose levels were significantly lower than the vehicle group.
After four injections, 14-hour fasting blood glucose levels were significantly reduced.
At 30 mg/kg, improved glucose tolerance and insulin sensitivity.
Even at 30 mg/kg, did not induce any detectable hepatotoxicity.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Research Protocol for Metabolic Diseases
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Research Protocol for Endocrine Diseases
- Mitochondrial membrane-potential and mitochondrial mass staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 170950-29-5
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Molecular Weight 354.40
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Formula C21H22O5
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SMILES
COC(C(OC)=CC=C1)=C1/C=C/C(/C=C/C2=C(C(OC)=CC=C2)OC)=O
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Synonyms
GO-Y015
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TrxR1-IN-B19 Related Classifications
HY-120914 Related Classifications
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