GSK3145095

Catalog No.S8845 Batch:S884501

Technical Data

Formula	C₂₀H₁₇F₂N₅O₂
Molecular Weight	397.38	CAS No.	1622849-43-7
Solubility (25°C)*	In vitro	DMSO	79 mg/mL (198.8 mM)
		Ethanol	6 mg/mL (15.09 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.)

Preparing Stock Solutions

Biological Activity

Description

GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.

Targets

RIP1 kinase ^[1]
(Cell-free assay)

6.3 nM

In vitro

GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinasedependent cellular responses. Highlighting its potential as a novel cancer therapy, the inhibitor is also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines U937 cells, L-cells NCTC 929 (L929) cells Concentrations 0-3 μM Incubation Time 5 h Method GSK3145095 is prepared in assay buffer and serially diluted 1:1.5 in a 22 point titration (high final concentration 3 μM) and added to a 384 white low volume Greiner plate. 3.5 μL of each inhibitor concentration and 3.5 μL of 25 nM enzyme (final) in assay buffer are added to the plate. Following these additions, 3.5 μL of ATP (15.6 μM to 875 μM final) in assay buffer is added to the plate to initiate the reaction. The reaction progresses for 5h at room temperature.

Cell Assay:^{^[1]}

Cell lines
U937 cells, L-cells NCTC 929 (L929) cells
Concentrations
0-3 μM
Incubation Time
5 h
Method
GSK3145095 is prepared in assay buffer and serially diluted 1:1.5 in a 22 point titration (high final concentration 3 μM) and added to a 384 white low volume Greiner plate. 3.5 μL of each inhibitor concentration and 3.5 μL of 25 nM enzyme (final) in assay buffer are added to the plate. Following these additions, 3.5 μL of ATP (15.6 μM to 875 μM final) in assay buffer is added to the plate to initiate the reaction. The reaction progresses for 5h at room temperature.

References

[1] Philip A Harris, et al. ACS Med Chem Lett. 2019 May 9;10(6):857-862.

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.