LIM Kinase (LIMK)

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.

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

LX7101 is a pyrrolopyrimidine-based, topically-delivered inhibitor of LIM domain kinase 2 (LIMK2), a kinase associated with the regulation of intraocular pressure.

R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1.

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

TH-263 is an inactive analog control for the type III allosteric LIM-kinase (LIMK) inhibitors TH-257, TH-255 and TH-251.

TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2.

DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. It exhibits high selectivity and potency, making it a strong candidate for the development of a chemical probe targeting CDK17 degradation.

DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity.

DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.

LIMK-IN-1 is a potent inhibitor of LIM-Kinase (LIMK), exhibiting IC50 values of 0.5 nM for LIMK1 and 0.9 nM for LIMK2. This compound is primarily utilized in research related to ocular hypertension and associated glaucoma, contributing to studies aimed at understanding the role of LIMK in these conditions. Its high specificity and efficacy make it a valuable tool for investigating the molecular pathways involved in ocular diseases.

CRT0105950 is a potent LIMK inhibitor, selectively targeting LIMK1 and LIMK2 with IC50 values of 0.3 nM and 1 nM, respectively. Its primary mechanism involves the inhibition of LIM kinases, which play a crucial role in regulating actin cytoskeleton dynamics and cell motility. This reagent is valuable for investigating tumor biology and potential therapeutic pathways in cancer research.

SR7826 is a potent and selective LIMK1 inhibitor, exhibiting an IC50 of 43 nM. This bis-aryl urea derivative demonstrates over 100-fold selectivity for LIMK1 compared to ROCK and JNK kinases. SR7826 serves as a valuable tool for investigating LIMK1-related signaling pathways and its role in cellular processes such as cytoskeletal dynamics and cancer progression.

TH470 is a highly selective inhibitor of LIMK1 and LIMK2, exhibiting IC50 values of 9.8 nM and 13 nM, respectively. This compound effectively modulates the actin cytoskeleton and related cellular processes by inhibiting LIM kinase activity. TH470 is particularly valuable in the study of orphan diseases and other conditions related to dysregulated LIMK signaling.

LIMK1 inhibitor BMS-4 is a selective inhibitor of LIM Kinases (LIMK1 and LIMK2). By inhibiting LIMK1, BMS-4 effectively blocks the phosphorylation of cofilin, a critical substrate, thereby modulating actin dynamics. It has demonstrated noncytotoxicity in A549 cells, making it a valuable tool for investigating LIMK-related pathways and their roles in cancer cell migration and invasion.

MDI-114215 is an allosteric inhibitor targeting LIM Kinase 1 and 2 (LIMK1/2). It effectively inhibits the phosphorylation of cofilin in induced pluripotent stem cells (iPSCs) derived from mouse brain regions. This compound shows potential applications in research related to Fragile X Syndrome (FXS), enabling investigations into cellular pathways affected by LIMK activity.

LIMK1 inhibitor 2 is a selective inhibitor of LIM kinase 1 (LIMK1), demonstrating an IC50 value of 9 μM. This compound effectively blocks LIMK1 activity, leading to the modulation of cytoskeletal dynamics. It is primarily utilized in research to investigate cellular processes such as cell migration, proliferation, and differentiation, contributing valuable insights into cancer biology and other related fields.

8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide is a sesquiterpene that acts as a selective inhibitor of LIMK1. By targeting this kinase, the compound effectively modulates cell motility, making it valuable for studies investigating cytoskeletal dynamics and cell migration. This reagent is applicable in various research contexts, including cancer metastasis and neurobiology, where LIMK1 plays a critical role.

LIMK-IN-3 is a potent inhibitor of LIMK2, demonstrating an IC50 of 1.2 nM. This compound exhibits significant inhibition of LIMK2 activity, which is crucial for understanding the role of LIMK2 in various cellular processes. LIMK-IN-3 is particularly relevant in glaucoma research, providing valuable insights into the molecular mechanisms underlying this condition.

LIJTF500025 is a potent and selective LIMK inhibitor that targets LIMK1 and LIMK2, exhibiting pIC50 values of 6.77 and 7.03, respectively, as determined by NanoBRET. This compound plays a crucial role in modulating actin dynamics and has potential applications in cancer research. Its ability to inhibit LIM kinase activity makes it a valuable tool for investigating the mechanisms underlying tumor progression and metastasis.

CRT 0105446 is a selective inhibitor of LIMK1, exhibiting an IC50 value of 8 nM. This compound is valuable for investigating the role of LIMK1 in cellular processes such as cytoskeletal dynamics and cell migration. Researchers can utilize CRT 0105446 to explore its effects in studies related to cancer, neurodegenerative diseases, and other conditions where LIMK1 modulation is implicated.

Curcolonol is a furan-type sesquiterpene that acts as an inhibitor of LIM kinase 1. It exhibits significant inhibitory activity against this target, making it a valuable compound for studying pathways involved in cancer progression. Curcolonol is particularly relevant for research applications in breast cancer, providing insights into potential therapeutic mechanisms and treatment strategies.

LIMK-IN-2 is a selective LIMK inhibitor that exhibits significant capacity to inhibit cell migration in osteosarcoma and cervical cancer cells. This compound demonstrates potential anti-angiogenic activity, making it a valuable tool for investigating the role of LIMK in cancer progression and therapeutic strategies. Research applications include studies focused on metastasis and the regulation of cellular motility in tumor biology.

LIMK1 Inhibitor 1 is a selective inhibitor of LIM domain kinase 1 (LIMK1), a critical regulator of actin cytoskeletal dynamics. This compound demonstrates potential anti-cancer activity by disrupting cancer cell migration and invasion. LIMK1 Inhibitor 1 is applicable in research focused on understanding the role of LIMK1 in oncogenesis and exploring therapeutic strategies for cancer treatment.