Khl 8430

Khl 8430 (6 μM; 15 min) reverses calmodulin (CaM)-induced inactivation of rabbit skeletal muscle phosphofructokinase (PFK), with an IC₅₀ of 1.6 μM. At a concentration of 6 μM, it restores PFK activity to a level above that observed in the absence of CaM. Furthermore, it binds to the CaM-PFK complex with a dissociation constant of 0.8 μM, thereby maintaining partial PFK activity in the ternary complex. At concentrations greater than 200 μM, it triggers non-specific, CaM-independent PFK inactivation^[1].
Khl 8430 (20 μM) completely inhibits the anti-calmodulin effect in fluorescence anisotropy assays using purified bovine brain calmodulin (CaM) and rabbit skeletal muscle phosphofructokinase (PFK), with an anti-CaM activity of 0% at a concentration of 20 μM^[2].
Khl 8430 (20 μM; 60 min preincubation with CaM, 20 min incubation with PFK) completely abolishes CaM-induced inactivation of rabbit skeletal muscle PFK, and exhibits 100% anti-CaM activity at a concentration of 20 μM^[2].
Khl 8430 (10-50 μM; 10-30 min) inhibits the activity of calmodulin (CaM)-activated bovine heart phosphodiesterase (PDE), and reduces its activity to near basal levels at concentrations as low as 10 μM^[1].
Khl 8430 (up to 300 μM) binds to the CaM-PFK ternary complex but does not displace rabbit skeletal muscle PFK from bovine brain CaM. This conclusion is supported by the observation that the fluorescence anisotropy of the CaM-PFK complex remains unchanged at concentrations up to 60 μM^[1].
Khl 8430 (up to 50 μM) binds to the CaM-PDE ternary complex but does not displace bovine heart PDE from bovine brain CaM; this is confirmed by the absence of changes in the fluorescence anisotropy of the CaM-PDE complex at concentrations up to 50 μM^[1].
Khl 8430 (200-600 μM) partially reverses the TFP-induced displacement of rabbit skeletal muscle PFK from bovine brain CaM, indicating negative cooperativity between Khl 8430 and TFP in binding to CaM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.