limk2

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.

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.

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.

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

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

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

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.

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.

THNAN69 is a potent chemical probe degrader specifically targeting LIMK2, with a DC50 value of 1 nM. This compound is useful for researching diseases driven by LIMK2 overexpression or dysregulation, such as cancer and ophthalmic conditions.

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.

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

DD-03-156 is a potent and selective degrader of CDK17 and LIMK2 . The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17 [1] .

DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in research on diseases or disorders caused by aberrant kinase activity [1].

FMF-06-098-1 is a multitargeted depressant that promotes the degradation of various kinases including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].

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.