LIM kinases (LIMKs) are important cell cytoskeleton regulators that play a prominent role in cancer manifestation and neuronal diseases. The LIMK family consists of two homologues, LIMK1 and LIMK2, which differ from one another in expression profile, intercellular localization, and function. The main substrate of LIMK is cofilin, a member of the actin-depolymerizing factor (ADF) protein family. When phosphorylated by LIMK, cofilin is inactive. LIMKs play a contributory role in several neurodevelopmental disorders and in cancer growth and metastasis.
LIM domain kinases (LIMK1 and 2) are substrate for Cdc42/Rac-PAK, and modulate actin dynamics by phosphorylating cofilin at serine-3. This modification inactivates cofilin’s actin severing and depolymerizing activity. LIMKs also translocate into the nucleus and regulate cell cycle progression. LIMKs are potential therapeutic targets for NF2 and other merlin-deficient tumors.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H2125 |
TH-257 |
2244678-29-1 | TH-257 (TH257) is a potent, selective, allosteric inhibitor of LIMK1 and LIMK2 with IC50 of 84 nM for LIMK1 and 39 nM for LIMK2 in a RapidFire MS assay; TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 uM; displays IC50 of 250 nM against ectopically expressed full-length LIMK1 and 150 nM LIMK2 in a life cell NanoBRET assay. |
H2124 |
T56-LIMKi |
924473-59-6 | A novel specific LIMK2 inhibitor; reduces phosphorylated cofilin (p-cofilin) by LIMK2 but not by LIMK1 and inhibits (IC50=30 uM) the proliferation in NF1−/− MEFs; synergizes with salirasib to destabilize the actin cytoskeleton, decreases anchorage-independent cell growth of NF1−/− MEFs; reduces tumor size and p-cofilin levels in a nude mouse Panc-1 xenograft model. |
H2123 |
SR7826 |
1219728-20-7 | SR7826 is a potent and selective LIM kinase (LIMK) inhibitor with IC50 of 43 nM, displays >100-fold selectivity over ROCK1 and ROCK2, as well as JNK kinases (>400-fold); inhibits only Limk1 and STK16 with >80% inhibition at 1 uM in a panel of 61 kinases; potently inhibits cofilin phosphorylation in A7r5, PC-3, and CEM-SS T cells (IC50 |
H2122 |
R-10015 |
2097938-51-5 | A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM ; exhibits good selectivity, with off-target inhibition of only LRRK2 and p70S6K (≥90% inhibition at 1 uM) and moderate inhibition of PKA (76%), ROCK2 (70%), and FLT3 (68%); blocks HIV-1 viral DNA synthesis, nuclear migration, and virion release; has broad-spectrum antiviral effect and inhibits multiple viruses, including EBOV, RVFV, VEEV, and HSV-1. |
H2121 |
Pyr-1 |
83947-94-8 | A novel potent, selective, cell permeable and ATP competitive LIMK inhibitor; stabilizes microtubules, induces a cell-cycle arrest at the S-G2–M phases, and blocks actin microfilament dynamics through inhibition of cofilin phosphorylation; blocks the invasion and proliferation of breast cancer cells, including paclitaxel-resistant cells, in vitro and tumor growth and metastasis in vivo in tumor xenograft. |
H2120 |
LX7101 |
1192189-69-7 | LX7101 is a potent, dual LIMK and ROCK inhibitor with IC50 of 4.3/32//69/32/ nM for LIMK2/LIMK1/ROCK1/ROCK2, respectively; kinase selectivity are eveluated in a panel of binding assays including 78 different receptors and transporters at Cerep (only 5 have >60% inhibition at 10 uM); demonstrates high efficacy in mouse model of ocular hypertension, ans shows potential for the treatment of glaucoma. |
H2119 |
LIMK1 and 2 dual inhibitor |
2215049-71-9 |
LIMK1 and 2 dual inhibitor is a potent, selective LIMK1/2 inhibitor with IC50 of <10 nM for both, 15-fold selectivity over B-Raf (IC50=10-100 nM); inhibits p-c-ofilin at Ser3 site, suppresses cell proliferation of MV-411 cell of with IC50 of 1-5 uM. |
H2118 |
LIMK-IN-22j |
1116571-01-7 | A potent, selective LIMK inhibitor with IC50 of 3.2 nM and 1.2 nM for LIMK1 and LIMK2, respectively; displays >100-fold selectivity for LIMK2 against ROCK1 and >900-fold selectivity against ROCK2; reduces intraocular pressure to baseline levels in a steroid induced mouse model of ocular hypertension (topical dosing). |
H2117 |
LIMK-IN-14 |
1116570-97-8 | A potent, selective LIMK inhibitor with IC50 of 0.9 nM and 0.5 nM and 1.2 nM for LIMK1 and LIMK2, respectively; displays >100-fold selectivity for LIMK2 against ROCK1 and >900-fold selectivity against ROCK2; reduces intraocular pressure to baseline levels in a steroid induced mouse model of ocular hypertension (topical dosing). |
H2116 |
CRT-0105950 |
1661845-86-8 | A novel potent LIMK inhibitor with IC50 of 0.3 nM and 1 nM for LIMK1 and LIMK2, respectively; inhibits cofilin phosphorylation and increase αTubulin acetylation in cells; shows significant sensitivity against 656 cancer cell lines, and rhabdomyosarcoma, neuroblastoma and kidney cancer cells (mean EC50=19.2 uM). |
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