STA-013
Based on 1 Customer Validation
STA-013 is a EphB tyrosine kinase inhibitor. STA-013 shows promising potency against EphB1 (IC50 = 0.69 µM), EphB2 (IC50 = 1.73 µM), and EphB4 (IC50 = 1.02 µM) tyrosine kinases. STA-013 results a inhibition of the EphB phosphorylated signal, coupled with increased p-AKT/AKT signaling, to suggest insulin signaling activation. STA-013 inhibits EphB tyrosine kinase by enhancing insulin receptor beta (IRβ) signaling, and decreasing TGF-β levels in the heart. STA-013 can be used for the study of type 2 diabetes and cardiac complications (diabetic cardiomyopathy).
For research use only. We do not sell to patients.
- Purity: 99.18%
- Formula: C24H17N3O2S
- Molecular Weight:411.48
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
More
Biological Activity
|
ErbB1 0.69 μM (IC50) |
ErbB2 1.73 μM (IC50) |
ErbB4 1.02 μM (IC50) |
STA-013 (5 µM) inhibits EphB1 (54%), EphB2 (42%), EphB4 (52%), SGK1 (47%), and PKBb (43%) without affecting the rest of 140 kinases via kinome profiling assay[1].
STA-013 (0.032-20 µM, 96 h) significantly inhibits lipid accumulation in a dose-dependent manner in the embryonic mouse 3T3-L1 cells[1].
STA-013 (1 µM, 30 min) results a significant reduction in basal respiration, proton leak, ATP production, and non-mitochondrial oxygen consumption, increases maximal respiration and spare respiratory capacity, exhibits a significant increase in glycolysis and glycolytic capacity and reduces palmitate oxidation in 3T3-L1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
STA-013 (12.5, 25 and50 mg/kg, i.p., daily for 6 weeks) induces weight loss not through reduced food intake or elevated metabolic rates in DIO mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:HFD (for 10 weeks) induced male C57BL/6J mice (16-20 weeks old)[1]
-
Dosage:12.5, 25 and 50 mg/kg
-
Administration:i.p., daily for 6 weeks
-
Result:Showed a significant reduction in whole-body weight, improved glucose clearance in the IP glucose tolerance test (GTT), and insulin sensitivity in the IP insulin tolerance test (ITT).
Showed a significant reduction in the fat mass associated with preserving the lean muscle mass in HFD-obese mice.
Induced intrascapular brown adipose tissue (BAT)-specific thermogenesis in HFD obese mice.
Showed significant reduction in whole-body weight associated with reduction in the fat mass (%) as well as increase in the lean mass (%), improved glucose clearance, and restored insulin sensitivity in HFD obese mice.
Inhibited phosphorylation of ephb tyrosine kinase forward signaling in both the liver and BAT at 25 mg/kg.
Increased the p-AKT/AKT signaling, which suggests the activation of insulin signaling in BAT and liver in HFD obese mice.
Increased insr-β protein levels compared to vehicle in BAT and liver lysates.
-
Animal Model:HFD (for 10 weeks) induced male C57BL/6J DIO mice (16-20 weeks old)[1]
-
Dosage:12.5, 25 and 50 mg/kg
-
Administration:i.p., daily for 6 weeks
-
Result:Significantly increased oxygen (VO 2 and carbon dioxide (VCO 2) consumption ) production in the light cycle.
Decreased profile in the respiratory exchange rates (RER) during the dark cycle.
Decrease in the total energy expenditure (EE) for STA- 013 treated HFD mice.
Induced weight loss occurred without a change in food intake, suggesting it was due to an elevated metabolic rate.
Chemical Information
-
Appearance Solid
-
Molecular Weight 411.48
-
Formula C24H17N3O2S
-
Color White to light yellow
-
SMILES
O=C(NCC1=CC=CC2=C1C=CN2C(C3=CC=CC=C3)=O)C4=CC5=CC=CN=C5S4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (60.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4303 mL | 12.1513 mL | 24.3025 mL | 60.7563 mL |
| 5 mM | 0.4861 mL | 2.4303 mL | 4.8605 mL | 12.1513 mL | |
| 10 mM | 0.2430 mL | 1.2151 mL | 2.4303 mL | 6.0756 mL | |
| 15 mM | 0.1620 mL | 0.8101 mL | 1.6202 mL | 4.0504 mL | |
| 20 mM | 0.1215 mL | 0.6076 mL | 1.2151 mL | 3.0378 mL | |
| 25 mM | 0.0972 mL | 0.4861 mL | 0.9721 mL | 2.4303 mL | |
| 30 mM | 0.0810 mL | 0.4050 mL | 0.8101 mL | 2.0252 mL | |
| 40 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5189 mL | |
| 50 mM | 0.0486 mL | 0.2430 mL | 0.4861 mL | 1.2151 mL | |
| 60 mM | 0.0405 mL | 0.2025 mL | 0.4050 mL | 1.0126 mL |