SGC-GAK-1

SGC-GAK-1

Biochem/physiol Actions

SGC-GAK-1 (CA93) is an ATP-competitive cyclin G-associated kinase (GAK) inhibitor (Ki = 3.1 nM by ATP site fluorescent tracer displacement assay; KD = 4.5 nM by ITC) that effectively inhibits Dengue viral entry and packaging in cultures (IC50 = 920 nM) without detectable cytotoxicity. SGC-GAK-1 exhibits much reduced affinity toward only 4 other kinases among a panel of ~400 (KD = 1.9 nM/GAK vs. 110 nM/RIPK2, 190 nM/ADCK3, 520 nM/NLK, 980 nM/AVCR1 by ligand competitive binding assay; IC50 = 110 nM/GAK vs. 360 nM/RIPK2 by cellular target engagement assay). SGC-GAK-1N (CA71) is a structure analog and the recommended negative control (GAK KD = 7.1 µM by ligand competitive binding assay; GAK & RIPK2 IC50 >50 µM by cellular target engagement assay). For characterization details of SGC-GAK-1, please visit the SGC-GAK-1 probe summary on the Structural Genomics Consortium (SGC) website.SGC-GAK-1N is the negative control for the active probe, SGC-GAK-1. SGC-GAK-1N is available from Sigma. To learn more about and purchase SGC-GAK-1N, click here.To learn about other SGC chemical probes, visit sigma.com/sgc

Features and Benefits

SGC-GAK-1 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575952 SGC-GAK-1 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£490.29 (exc VAT) per 25MG
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3575953 SGC-GAK-1 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£142.07 (exc VAT) per 5MG
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