2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. LIM Kinase (LIMK)

LIM Kinase (LIMK)

LIMKs

LIM Kinase (LIMK)

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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.

LIM Kinase (LIMK) Isoform Specific Products:

LIM Kinase (LIMK) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-136848
    SM1-71
    		Inhibitor
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit 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 inhibit proliferation of multiple cancer cell lines.
    SM1-71
  • HY-18305
    BMS-5
    		Inhibitor 99.51%
    BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
    BMS-5
  • HY-18304
    BMS-3
    		Inhibitor 99.46%
    BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.
    BMS-3
  • HY-12659
    LX7101
    		Inhibitor 99.75%
    LX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research.
    LX7101
  • HY-122630
    TH-257
    		Inhibitor 98.01%
    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. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.
    TH-257
  • HY-159897
    PAK4-IN-5
    		Inhibitor
    PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.).
    PAK4-IN-5
  • HY-12659B
    LX7101 monohydrochloride
    		Inhibitor
    LX7101 monohydrochloride is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 monohydrochloride proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 monohydrochloride has the potential for ocular hypertension and associated glaucoma research.
    LX7101 monohydrochloride
  • HY-148062
    RSS0680
    		98.03%
    RSS0680 (Example 22) is a bifunctional compound targeted protein degradation of kinases. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used for research of disease or disorder mediated by aberrant kinase activity.
    RSS0680
  • HY-19353
    SR7826
    		Inhibitor 99.30%
    SR7826 is a class of bis-aryl urea derived potent, selective and orally active LIM kinase (LIMK) inhibitor with an IC50 of 43 nM for LIMK1. SR7826 is >100-fold more selective for LIMK1 than ROCK and JNK kinases.
    SR7826
  • HY-148063
    DB0614
    		98.80%
    DB0614 is a PROTAC based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade 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. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity.(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))
    DB0614
  • HY-137346
    DD-03-156
    		Degrader 99.63%
    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 (Blue: VHL ligand (HY-112078), Black: linker HY-124380 (HY-124380)；Pink: BRAF inhibitor (HY-14660)).
    DD-03-156
  • HY-19352
    T56-LIMKi
    		Inhibitor 99.07%
    T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.
    T56-LIMKi
  • HY-148061
    DB1113
    		99.28%
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades 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. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity.
    DB1113
  • HY-120025
    CRT0105950
    		Inhibitor 99.91%
    CRT0105950 is a potent LIMK inhibitor, with IC50s of 0.3 nM and 1 nM for LIMK1 and LIMK2 respectively. CRT0105950 can be used for the research of cancer.
    CRT0105950
  • HY-120097
    R-10015
    		Inhibitor 99.72%
    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.
    R-10015
  • HY-151539
    TH470
    		Inhibitor 99.57%
    TH470 is a highly selective LIMK1/2 (LIM kinase1/2) inhibitor (LIMK1 IC50=9.8 nM; LIMK2 IC50=13 nM), and can be used in orphan disease research.
    TH470
  • HY-128062
    LIMK1 inhibitor BMS-4
    		Inhibitor ≥99.0%
    LIMK1 inhibitor BMS-4 is a LIM Kinase (LIMK) inhibitor targeting to LIMK1/2. LIMK1 inhibitor BMS-4 inhibits phosphorylation of cofilin, the LIMK substrate. However, LIMK1 inhibitor BMS-4 is noncytotoxic on A549 cells.
    LIMK1 inhibitor BMS-4
  • HY-14227
    LIMK-IN-1
    		Inhibitor 99.33%
    LIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. LIMK-IN-1 can be used for ocular hypertension and associated glaucoma research.
    LIMK-IN-1
  • HY-N10868
    8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide
    		Inhibitor
    8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility.
    8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide
  • HY-123345
    CRT 0105446
    		Inhibitor
    CRT 0105446 (compound 22d) is a LIMK1 inhibitor, with an IC50 of 8 nM.
    CRT 0105446
Cat. No. Product Name / Synonyms Application Reactivity
LIM Kinase (LIMK) Isoform Comparison

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