2,3-Butanedione monoxime (BDM) chemically removes phosphate groups from many proteins, and its action on DRK1 channels was examined after expression of DRK1 cRNA in Xenopus oocytes. In two-microelectrode voltage-clamp experiments, the application of 2,3-Butanedione monoxime to the bath inhibited DRK1 current (ki = 16.6 mM, H = 0.96) rapidly and reversibly, with a time course similar to the time course of solution change within the bath. DRK1 current was inhibited at all potentials; the time course of current activation, deactivation and inactivation were unaffected by 2,3-Butanedione monoxime. In inside-out patch-clamp experiments, the application of 2,3-Butanedione monoxime to the cytoplasmic surface similarly inhibited channel activity rapidly and reversibly (ki = 10.7 mM, H = 1.01) in the absence of rephosphorylating substrates. These results are inconsistent with a phosphatase effect, because such an effect should be irreversible in cell-free, ATP-free patches. Instead, the results suggest that 2,3-Butanedione monoxime can inhibit DRK1 channels directly from inside or outside of the membrane.
Molecular Weight | 101.1 |
Formula | C4H7NO2 |
CAS Number | 57-71-6 |
Solubility (25°C) | DMSO ≥ 30 mg/mL |
Storage | 2-8°C, dry, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Arthur Forer, et al. Does 2,3-butanedione monoxime inhibit nonmuscle myosin?
[5] L C Sellin, et al. Multiple effects of 2,3-butanedione monoxime
Related Myosin Products |
---|
Myosin Light Chain Kinase Substrate (smooth muscle)
Myosin Light Chain Kinase Substrate (smooth muscle) is a smooth muscle myosin light chain kinase (MLCK) synthetic peptide substrate. |
Kemptamide
Kemptamide, a 13 amino acid fragment with a sequence corresponding to residues 11-23 of gizzard light chain. |
MYK-224
MYK-224 is a cardiac myosin complex modulator that can be used in studies related to cardiovascular disease. |
Myosin V-IN-1
Myosin V-IN-1 is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. |
16-38-Thymosin β4 (cattle) TFA
16-38-Thymosin β4 (cattle) TFA is a non-Ca2+-dependent MLCK activator with high affinity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.