lim kinase (limk)

Aurora/LIM kinase-IN-1 (Compound F114) is a potent aurora and lim kinase dual inhibitor. Aurora/LIM kinase-IN-1 inhibits the proliferation and invasion of GBM that may be used in drug development efforts for GBM, furthermore other cancers. Aurora kinases and lim kinases are the kinases which involved in neoplastic cell division and cell motility, respectively [1].

BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.

R-10015 is a highly potent and selective LIMK inhibitor that blocks LIMK by binding to the ATP-binding pocket. It inhibits human LIMK1 with an IC50 value of 38 nM. It also exerts broad-spectrum antiviral effects and may be used in HIV infection research.

S3 Fragment is a biologically active peptide featuring the amino-terminal phosphorylation site unique to Xenopus ADF/cofilin, which is the target of LIM kinase (LIMK) phosphorylation. LIMK1, a pivotal regulator of the actin cytoskeleton, phosphorylates ADF/cofilin at serine-3, leading to its inactivation. As a segment of the S3 peptide harboring the serine-3 sequence, this fragment serves as a widely recognized competitive inhibitor of LIMK1.

BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.

TH-257 is a Potent and selective allosteric LIMK 1/2 inhibitor(LIMK1 and LIMK2, IC50 of 84 nM and 39 nM).

T56-LIMKi (T5601640) is a selective inhibitor of LIMK2.

LX7101 is a potent inhibitor of both LIM kinase (LIMK) 1 and 2, and Rho-associated kinase 1 (ROCK1) and ROCK2, with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, demonstrated by its lack of cross-reactivity in a panel of binding assays involving 78 receptors, transporters, and an additional 430 kinases, at a concentration of 10 μM. The topical administration of LX7101 (3 μl of a 1 mg/ml solution) to the eye has been shown to reduce intraocular pressure in a dexamethasone-induced mouse model of glaucoma.

LIMK1 inhibitor BMS-4 is a compound targeting LIM Kinase (LIMK) 1/2, specifically inhibiting the phosphorylation of its substrate, cofilin, but it remains noncytotoxic on A549 cells.