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Description: BMS-5, also known as LIMKI-3, is an analog of BMS-3 and potent inhibitor of the LIM kinase (LIMK) with IC50 values of 7 and 8 nM for LIMK1 and LIMK2 respectively. BMS-5 inhibits cofilin-Ser3 phosphorylation in a dose-dependent manner in Nf2deltaEx2mouse Schwann cells (MSCs) with an IC50 of ca.2 uM. Inhibition of LIMK1 by specific inhibitors (BMS-5) resulted in lower levels of actin polymerization during capacitation and a dramatic decrease in the percentage of sperm that undergo acrosomal exocytosis. Thus, we demonstrated for the first time that the master regulators of actin dynamics in somatic cells are present and active in mouse sperm. Combining the results of our present study with other results from the literature, we have proposed a working model regarding how LIMK1 and Cofilin control acrosomal exocytosis in mouse sperm.
Reference: Dev Biol. 2015 Sep 15; 405(2):237-49; Mol Cancer Ther. 2008 Nov; 7(11):3490-8.
Related CAS #: 1338247-30-5 (BMS-3)
Chemical Name: N-[5-[1-(2, 6-Dichlorophenyl)-3-(difluoromethyl)-1H-pyrazol-5-yl]-2-thiazolyl]-2-methylpropanamide
InChi Key: IVUGBSGLHRJSSP-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H14Cl2F2N4OS/c1-8(2)16(26)23-17-22-7-13(27-17)12-6-11(15(20)21)24-25(12)14-9(18)4-3-5-10(14)19/h3-8, 15H, 1-2H3, (H, 22, 23, 26)
SMILES Code: CC(C)C(NC1=NC=C(C2=CC(C(F)F)=NN2C3=C(Cl)C=CC=C3Cl)S1)=O
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