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SCH-202676 | DDX1 & DDX41 Inhibitor

$129.00$349.00

SCH-202676  is a DDX1 and DDX41 inhibitor that has been fully validated using the Transcreener ADP Assay. An IC50 of 0.86 µM (DDX1) 1.78 µM (DDX41)was obtained using a 12-point dose-response assay. Contact us for bulk sizes.

SKU: 5002-5mg , 5002-25mg Category: Tag:

Technical Data for SCH-202676

Functional Activity with Human DDX1

Activity was measured using the Transcreener® ADP2 FP Assay using 12 nM human DDX1 (BellBrook Labs #2305). SCH-202676 was serially diluted and incubated with enzyme for 30 minutes. The following was added to start the reaction: 15 µM ATP, 0.5 mg/mL yeast RNA, 50 mM TRIS pH 7.5, 2 mM MgCl2, 0.01% Triton X-100; 10 μL Enzyme Reaction incubated @ 30°C for 60 minutes in a Corning® low-volume 384-well plate (#4514). 10 μL of the following detect mix was added: 16 μg/ mL ADP2 Ab, 4 nM ADP2 Tracer, 1X Stop and Detect Buffer B. 20 μL Complete Reaction was incubated for 60 minutes and read on a CLARIOstarPlus instrument. Fluorescent Polarization values were converted to ADP formed with a 10 μM ADP Standard Curve and was plotted using Prism (GraphPad). An IC50 of 0.86 µM was obtained.

SCH-202676 Dose-Response with DDX1

IC50 = 0.86 µM

Functional Activity with Human DDX41

Activity was measured using the Transcreener® ADP2 FP Assay using 100 nM human DDX41 (BellBrook Labs #2315). SCH-202676 was serially diluted and incubated with enzyme for 30 minutes. The following was added to start the reaction: 15 µM ATP, 0.5 mg/mL yeast RNA, 50 mM TRIS pH 7.5, 2 mM MgCl2, 0.01% Triton X-100; 10 μL Enzyme Reaction incubated @ 30°C for 60 minutes in a Corning® low-volume 384-well plate (#4514). 10 μL of the following detect mix was added: 16 μg/ mL ADP2 Ab, 4 nM ADP2 Tracer, 1X Stop and Detect Buffer B. 20 μL Complete Reaction was incubated for 60 minutes and read on a CLARIOstarPlus instrument. Fluorescent Polarization values were converted to ADP formed with a 10 μM ADP Standard Curve and was plotted using Prism (GraphPad). An IC50 of 1.78 µM was obtained.

SCH-202676 Dose-Response with DDX41

IC50 = 1.78 µM

Learn More About the Transcreener ADP Assay to Measure SCH-202676 Inhibition

Detailed Description

In addition to inhibiting ATPase activity of DDX1 and DDX41, SCH-202676 is a reversible inhibitor of both agonist and antagonist binding to G protein-coupled receptors (GPCRs).1  IC50’s = 0.1-1.7 µM for nine GPCRs.1  Modification of GPCRs is accomplished via sulfhydryl modification.2,3

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References

  1. Fawzi et al. (2001) SCH-202676: an allosteric modulator of both agonist and antagonist binding to G protein-coupled receptors. Mol.Pharmacol. 59 30.
  2. Lewandowicz et al. (2006) The ‘allosteric modulator’ SCH-202676 disrupts G protein-coupled receptor function via sulphydryl-sensitive mechanisms  Br.J.Pharmacol. 147 422
  3. Goblyos et al. (2005) Synthesis and biological evaluation of a new series of 2,3,5-substituted[1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action J.Med.Chem. 48 1145
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