To understand the physiological implication of inhibiting the LIMK/Cofilin signaling pathway in sperm physiology, we demonstrated that inhibition of pLIMK1 with BMS-3 resulted in low levels of F-actin. What is the relative contribution of RhoA/C and Rac1 during capacitation is still unknown. Another important aspect to determine is how the LIMK1/Cofilin signaling pathway interacts with PLD1, which was shown to be essential for actin polymerization in bovine sperm. One interesting possibility is that pCofilin stimulates PLD1 activity as demonstrated recently
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||30 mg/mL in DMSO|
PKA-dependent phosphorylation of LIMK1 and Cofilin is essential for mouse sperm acrosomal exocytosis.
Romarowski A, et al. Dev Biol. 2015 Sep 15;405(2):237-49. PMID: 26169470.
VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, with a Kd value of 80 to 90 nM.
6-Methylcoumarin belongs to the class of organic compounds known as coumarins and derivatives.
BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
Ezutromid (also known as BMN-195 and SMT C1100) is a first orally bioavailable utrophin's translation modulator with EC50 of 0.4 uM.
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
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