lim kinase

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

LIMK-IN-22j (LIMK inhibitor 22j) is an effective and selective inhibitor of LIMK.

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

BMS-5 (LIMKi 3) is a highly potent LIMK inhibitor, exhibiting IC50 values of 7 nM for LIMK1 and 8 nM for LIMK2.

Aurora LIM kinase-IN-1 (Compound F114) is a potent dual inhibitor of aurora and LIM kinases. It inhibits the proliferation and invasion of glioblastoma multiforme (GBM), making it a potential candidate for drug development in GBM and other cancers. Aurora and LIM kinases are involved in neoplastic cell division and cell motility, respectively [1].

LX-7101 hydrochloride is a potent LIMK and ROCK2 inhibitor with antihypertensive activity, inhibits LIMK1 2, ROCK, PKA, and can be used to study glaucoma.

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.

BMS-3 is a potent LIMK inhibitor with IC50 values 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).

LY2812223 is a highly effective and functionally selective mGlu2 receptor agonist. It has a mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).

CRT-0105950 is a potent LIMK inhibitor with high affinity for both LIMK1 and LIMK2.CRT-0105950 inhibits filamentous cutin phosphorylation and promotes α-microtubulin acetylation in cells.CRT-0105950 can be used in the study of renal carcinoma.

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1 2 3 4 6 7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A B, MAPK1 3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.

Damnacanthal is a natural anthraquinone compound with potential anticancer, anti-inflammatory, antioxidant, anti-malarial, and antiviral effects.Damnacanthal inhibits a variety of protein kinases such as LIMK1 (IC50=0.8 μM), LIMK2 (IC50=1.5 μM), and Lck (IC50=17 nM), and inhibits the growth of human hepatocellular carcinoma (SKHep-1) and human breast cancer (MCF-7) cells.

Narciclasine (Lycoricidinol), a natural product, modulates the Rho Rho-kinase LIM kinase cofilin signaling pathway, greatly increasing GTPase RhoA activity.

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

TH470, a potent and highly selective inhibitor of LIM kinase 1 2 (LIMK1 2), demonstrates specificity with IC50 values of 9.8 nM for LIMK1 and 13 nM for LIMK2, making it applicable in orphan disease 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.

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.

Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin phospho-myosin II co-aggregates by stimulation of the RhoA ROCK pathway and inhibition of LIM-Kinase.