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
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Molecular Weight | 429.27 |
Formula | C17H12Cl2F2N4OS |
CAS Number | 1338247-30-5 |
Form | Solid |
Solubility (25°C) | DMSO ≥ 50 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility. |
LIMK-IN-1
LIMK-IN-1 is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. |
Curcolonol
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CRT0105950 is a potent LIMK inhibitor, with IC50s of 0.3 nM and 1 nM for LIMK1 and LIMK2 respectively. CRT0105950 can be used for the research of cancer. |
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