Description
BTS is an inhibitor of skeletal muscle myosin II ATPase activity that reduces the affinity of ADP-myosin for actin. It inhibits calcium-stimulated ATPase activity of rabbit muscle myosin subfragment 1 (S1) in an actin-independent manner with an IC
50 value of approximately 5 μM. It is selective for calcium-stimulated myosin II over human platelet myosin II, kinesin, pyruvate kinase, and lactate dehydrogenase at 100 μM. BTS (2 μM) inhibits the activity of skeletal muscle myosin, reversibly reducing the sliding velocity of heavy meromyosin in a gliding-filament assay. It inhibits isometric calcium-activated tension in isolated fast-twitch rabbit psoas muscle fibers (IC
50 = ~3 μM) but not in isolated slow-twitch rat trabeculae and papillary cardiac muscle. BTS is also an intermediate in the synthesis of sulfonamides.
Chemical Properties
White Solid
Uses
A potent inhibitor of skeletal muscle Ca2+-stimulated myosin S1 ATPase (IC50 approx. 5uM) activity. Reversible blocks the gliding motility. Also weakens myosin interaction with F-actin. Does not affect platelet myosin II
Uses
A potent inhibitor of calcium-stimulated myosin S1 ATPase
Definition
ChEBI: 4-methyl-N-(phenylmethyl)benzenesulfonamide is a sulfonamide.
Synthesis Reference(s)
The Journal of Organic Chemistry, 28, p. 592, 1963
DOI: 10.1021/jo01037a523
Biological Activity
Selective inhibitor of the ATPase activity of skeletal muscle myosin II subfragment 1 (S1) (IC 50 ~ 5 mM). Reversibly blocks gliding motility and suppresses force and twitch production in fast skeletal muscle.