limk1

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).

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.

TH-263 is inactive toward both LIMK1 and LIMK2 and thus can be used as negative control for TH-257, and is a diaryl sulfonamide derivative.

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.

AWL-II-38.3 is a highly potent EphA3 inhibitor with potent kinase inhibitory activity against EphA3 but no significant cellular activity against Src family kinases or b-raf.

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

BMS-3 is a potent LIMK inhibitor with IC50 values of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.

LIMK1 inhibitor 2 is a LIMK1 inhibitor with an IC50 value of 9 μM.

LIMK1 inhibitor1 (compound 24) is a LIMK1 inhibitor, potentially useful for cancer research.

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.

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.

SM311 (Compound 10) is a potent, selective, and irreversible inhibitor of LIMK1, with an EC50 of 0.045 μM and over 30-fold selectivity for LIMK1 over LIMK2. It can inhibit cofilin phosphorylation and actin cytoskeleton regulation. SM311 shows potential for research in neurodegenerative disorders such as Fragile X Syndrome (FXS) and Alzheimer's disease, as well as in tumor invasion.

MDI-117740 is a dual LIMK1/2 inhibitor. It demonstrates strong cellular target binding in HEK293 cells, inhibiting LIMK1 (pIC50=6.73) and LIMK2 (pIC50=7.18). In MDA-MB-231 cells, MDI-117740 shows significant anti-migratory activity. This compound is useful for studying diseases associated with LIMK dysregulation, such as cancer and neurodegenerative disorders.

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

SR7826 is a selective LIMK inhibitor.

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

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.

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.

PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).

MDI-114215 (compound 85) serves as an allosteric dual inhibitor of LIMK1/2 and exhibits favorable in vivo tolerance. It is capable of inhibiting the phosphorylation of cofilin in mouse brain region-induced pluripotent stem cells (iPSCs) and can be utilized in Fragile X Syndrome (FXS) research.

SPU-106 is a novel specific PAK4 inhibitor, effectively inhibiting the invasion of SGC7901 cells without cytotoxicity, regulating the PAK4/LIMK1/cofilin and PAK4/SCG10 signaling pathways.

TH251 is a highly selective antagonist of LIMK1 and LIMK2 (LIMK1/2).

DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. This capability positions DB1113 as a valuable tool for research into diseases or disorders associated with aberrant kinase activity [1].