SU1498

Catalog No.S6535 Batch:S653501

Technical Data

Formula	C₂₅H₃₀N₂O₂
Molecular Weight	390.52	CAS No.	168835-82-3
Solubility (25°C)*	In vitro	DMSO	78 mg/mL (199.73 mM)
		Ethanol	78 mg/mL (199.73 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells.

Targets

KDR ^[1]

In vitro

SU1498 accentuates accumulation of phosphorylated ERK in endothelial cells and inhibits its kinase activity while having no effect on phosphorylation of Akt. SU1498 does not affect phospho-ERK translocation to nucleus^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HUVECs Concentrations 10 μM Incubation Time 15 min Method Cells are inoculated into the wells of 6-well culture plates (3 × 10⁵ cells/well) and grown for 16 h in DMEM-based medium at 37 °C in the atmosphere of 5% CO2. After an overnight starvation (0.5% fetal bovine serum), the medium is removed, and the cells are washed with PBS and overlaid with 0.4 ml of DMEM. From this point on, all incubations are done at 25 °C. The inhibitors (SU1498, 10 μM; AG1433, 10 μM; AG1296, 25 μM; PD153035, 1 μM) are added and followed 15 min later by the growth factors: SPP, 1 μm; VEGF, 100 ng/ml; HGF, 100 ng/ml; bFGF, 10 ng/ml; EGF, 10 ng/ml. Forskolin (10 μm), a gratuitous inducer of adenylyl cyclase, is used as a control because of its known ability to enhance ERK phosphorylation. After a 10-min incubation, the medium is siphoned off, and the cells are lysed with 100 μl of lysis buffer. Samples (10 μl) of each lysate are fractionated by SDS-PAGE, and proteins are transferred to nitrocellulose and probed with anti-phospho-Akt or anti-phospho-ERK1/2 antibody. To show comparable loading, anti-actin antibody is used.

Cell Assay:^{^[1]}

Cell lines
HUVECs
Concentrations
10 μM
Incubation Time
15 min
Method
Cells are inoculated into the wells of 6-well culture plates (3 × 10⁵ cells/well) and grown for 16 h in DMEM-based medium at 37 °C in the atmosphere of 5% CO2. After an overnight starvation (0.5% fetal bovine serum), the medium is removed, and the cells are washed with PBS and overlaid with 0.4 ml of DMEM. From this point on, all incubations are done at 25 °C. The inhibitors (SU1498, 10 μM; AG1433, 10 μM; AG1296, 25 μM; PD153035, 1 μM) are added and followed 15 min later by the growth factors: SPP, 1 μm; VEGF, 100 ng/ml; HGF, 100 ng/ml; bFGF, 10 ng/ml; EGF, 10 ng/ml. Forskolin (10 μm), a gratuitous inducer of adenylyl cyclase, is used as a control because of its known ability to enhance ERK phosphorylation. After a 10-min incubation, the medium is siphoned off, and the cells are lysed with 100 μl of lysis buffer. Samples (10 μl) of each lysate are fractionated by SDS-PAGE, and proteins are transferred to nitrocellulose and probed with anti-phospho-Akt or anti-phospho-ERK1/2 antibody. To show comparable loading, anti-actin antibody is used.

References

[1] Boguslawski G, et al. J Biol Chem. 2004, 279(7):5716-24.

Selleck's SU1498 has been cited by 2 publications

Low-Dose Sorafenib Acts as a Mitochondrial Uncoupler and Ameliorates Nonalcoholic Steatohepatitis. [ Cell Metab, 2020, 5;31(5):892-908 e11]	PubMed: 32375062
[ Biol Open, 2018, ]	PubMed: 30232195

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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