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.
Humanized vascular endothelial growth factor (VEGF) antibody (bevacizumab; Avastin) is a highly effective monoclonal antibody against metastatic colorectal cancer and several other advanced late stage cancers.
MCC950 is a potent, selective NLRP3 inhibitor with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.
MAK683, an epigenetic drug for nasopharyngeal carcinoma, which is more prevalent in China than elsewhere, has entered Phase I clinical trials.
MTX-211 is a enamide hydrate.
GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain.
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