2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Metabolic Enzyme/Protease
  3. EGFR Akt Mitochondrial Metabolism
  4. STA-013

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.

STA-013

STA-013 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
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200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

STA-013 Related Antibodies

Top Publications Citing Use of Products

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All Akt Isoform Specific Products:

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1].

IC50 & Target[1]

ErbB1

0.69 μM (IC50)

ErbB2

1.73 μM (IC50)

ErbB4

1.02 μM (IC50)

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax AUC F C0 T1/2 (Metabolic) AUCinf CL Vss_obs
Mice[1] 25 mg/kg i.p. 1126 ng/mL 0.35 h 0.158 mL/min 0.75 / / / / /
Mice[1] 25 mg/kg i.v. / / / / 1404 ng/mL 16.10 h 0.212 mL/min 10.50 L/h/kg 88.8 L/kg
In Vivo

STA-013 (12.5, 25 and 50 mg/kg, i.p., daily for 6 weeks) promotes weight loss, improves glucose clearance and insulin sensitivity, and enhances insulin signaling in isolated brown adipose tissue and liver in high-fat diet-induced C57BL/6J mice. In these obese mice [1].
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.
Molecular Weight

411.48

Formula

C24H17N3O2S
Appearance

Solid

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4303 mL 12.1513 mL 24.3025 mL
5 mM 0.4861 mL 2.4303 mL 4.8605 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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STA-013 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STA-013STA013STA 013EGFRAktMitochondrial MetabolismEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BEphBglucose homeostasisinsulin resistanceTGF-βtype 2 diabetescardiac complicationsInhibitorinhibitorinhibit

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