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Entospletinib

Manufactured by Gilead Sciences
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Entospletinib is a laboratory reagent used for research purposes. It is a small molecule inhibitor that targets the spleen tyrosine kinase (SYK) enzyme. SYK plays a role in various cellular processes and is of interest in biomedical research.

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Lab products found in correlation

Ibrutinib, by Selleck Chemicals (2 mentions) Gs 5829, by Gilead Sciences (2 mentions) Idelalisib, by Gilead Sciences (2 mentions) Adenosine triphosphate (atp), by Thermo Fisher Scientific (1 mentions) Mitotempo, by Merck Group (1 mentions) Nigericin, by Merck Group (1 mentions) Mcc950, by Merck Group (1 mentions) Dimethyl sulfoxide (dmso), by Merck Group (1 mentions) Fostamatinib, by Selleck Chemicals (1 mentions) Dasatinib, by Selleck Chemicals (1 mentions) Selumetinib, by Selleck Chemicals (1 mentions)

4 protocols using entospletinib

1

Inhibitor-based Cellular Assays

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GS-5829, the PI3Kδ inhibitor idelalisib, and the SYK inhibitor entospletinib were provided by Gilead Sciences, Inc. (Foster city, CA, USA) as 10 mM solutions in dimethyl sulfoxide (DMSO). JQ1 and the BTK inhibitor ibrutinib were purchased from Selleck Chemicals (Houston, TX, USA).
Kim E., ten Hacken E., Sivina M., Clarke A., Thompson P.A., Jain N., Ferrajoli A., Estrov Z., Keating M.J., Wierda W.G., Bhalla K.N, & Burger J.A. (2019). The BET Inhibitor GS-5829 Targets Chronic Lymphocytic Leukemia Cells and Their Supportive Microenvironment. Leukemia, 34(6), 1588-1598.
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2

Inflammasome Activation in Macrophages

Cited 1 time
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Culture medium of differentiated macrophages was exchanged after 5 days of incubation. For inhibitor experiments, cells were preincubated with either 0.1% DMSO (Merck, KGaA, Darmstadt, Germany), MCC950 (10 μM) (Merck), KINK‐1 (5 μM) (Merck), MitoTEMPO (10 μM) (Merck), entospletinib (5 μM) (Gilead Sciences, Inc., Foster City, CA, USA), or tamatinib/R406 (5 μM) (InvivoGgen, San Diego, CA, USA) in RPMI medium for 2 h at 37°C and 5% CO2. Thereafter or without inhibitors, cells were stimulated with lipopolysaccharide (LPS) (5 μg/ml) (Merck) or SARS‐CoV‐2 spike protein (0.1 μg/ml) and incubated for 4 h at 37°C and 5% CO2 to prime the inflammasome process. Inflammasome activation and IL‐1β secretion were initiated by addition of nigericin (5 μM) (Merck) or ATP (5 mM) (Thermo Fisher) and the cells were further incubated for 2 h (Theobald et al, 2021 (link)).
Theobald S.J., Simonis A., Mudler J.M., Göbel U., Acton R., Kohlhas V., Albert M., Hellmann A., Malin J.J., Winter S., Hallek M., Walczak H., Nguyen P., Koch M, & Rybniker J. (2022). Spleen tyrosine kinase mediates innate and adaptive immune crosstalk in SARS‐CoV‐2 mRNA vaccination. EMBO Molecular Medicine, 14(8), e15888.
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3

Inhibitor-based Cellular Assays

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GS-5829, the PI3Kδ inhibitor idelalisib, and the SYK inhibitor entospletinib were provided by Gilead Sciences, Inc. (Foster city, CA, USA) as 10 mM solutions in dimethyl sulfoxide (DMSO). JQ1 and the BTK inhibitor ibrutinib were purchased from Selleck Chemicals (Houston, TX, USA).
Kim E., ten Hacken E., Sivina M., Clarke A., Thompson P.A., Jain N., Ferrajoli A., Estrov Z., Keating M.J., Wierda W.G., Bhalla K.N, & Burger J.A. (2019). The BET Inhibitor GS-5829 Targets Chronic Lymphocytic Leukemia Cells and Their Supportive Microenvironment. Leukemia, 34(6), 1588-1598.
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4

Selective SYK Inhibitor Entospletinib Protocol

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The selective SYK inhibitor entospletinib (ENTO)32 (link) was provided as a dispersible powder for in vitro studies and in rodent chow formulation in 0.03%, 0.05%, and 0.07% concentrations for in vivo animal studies by Gilead Sciences Inc. (Foster City, CA, USA). Rodent chow concentrations were selected and optimized based upon PK levels achieved in ENTO-treated adult patients with acute leukemia (clinicaltrials.gov identifiers: NCT02404220 and NCT02343939).33 Vincristine and dexamethasone were purchased from the Children’s Hospital of Philadelphia investigational pharmacy (Philadelphia, PA, USA). The MEK inhibitor selumetinib, SYK inhibitor fostamatinib, and multi-kinase inhibitor dasatinib were purchased from Selleckchem (Houston, TX, USA) or LC Labs (Woburn, MA, USA). Cell viability and phosphoflow cytom etry signaling analyses of human B-ALL cell lines and PDX model cells treated with vehicle, kinase inhibitors, or chemotherapy (in vitro or in vivo) are detailed in the Online Supplementary Methods with data shown in Online Supplementary Figures S1-S6.
Loftus J.P., Yahiaoui A., Brown P.A., Niswander L.M., Bagashev A., Wang M., Shauf A., Tannheimer S, & Tasian S.K. (2020). Combinatorial efficacy of entospletinib and chemotherapy in patient-derived xenograft models of infant acute lymphoblastic leukemia. Haematologica, 106(4), 1067-1078.
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