LX7101

SKU: orb1707047

Description

LX7101 is a potent small molecule inhibitor with high selectivity for LIMK1, LIMK2, and ROCK2, and it also potently inhibits PKA. This compound is a valuable research tool for studying cytoskeletal dynamics, cell motility, and neuronal morphology in both cellular and animal models of disease.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1192189-69-7
• MW: 451.52
• Purity: 99.08% (May vary between batches)
• Formula: C₂₃H₂₉N₇O₃
• SMILES: CN(C)C(=O)Oc1cccc(NC(=O)C2(CN)CCN(CC2)c2ncnc3[nH]cc(C)c23)c1
• Target: ROCK,PKA,LIM Kinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.07 mM);DMSO:150 mg/mL (332.21 mM)

Bioactivity

• Target IC50:
  LIMK2:1.6 nM|PKA:1 nM|ROCK2:10 nM|LIMK1:24 nM
• In Vivo:
  Topical doses of LX-7101 are evaluated for tolerability in the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single-dose studies. LX-7101 is advanced to Phase-I clinical trials as intraocular pressure (IOP)-lowering agent for the treatment of glaucoma. LX-7101 shows a significant IOP reduction at time points ranging from 1 h to 6 h post-administration in rabbits. LX-7101 (5%) achieved an additional reduction of IOP (5.0 mmHg total reduction) compared to the 0.1% formulation. It also demonstrated a long duration of action, in the mouse IOP assay, with IOP not returning to baseline until more than 8 h postdose.
• In Vitro:
  LX7101 is a dual LIM-kinase and ROCK inhibitor for treating ocular hypertension and associated glaucoma, showing effective inhibition of Akt1 (IC50<1 nM). Its primary activity is due to LIMK2 inhibition under physiological conditions, with enhanced selectivity for LIMK2 at higher physiological ATP concentrations.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LX7101, LX-7101, LX 7101, inhibit, LIM Kinase, LIMK2, LIMK1, LIMKinase, Inhibitor, ROK, ROCK, ROCK2, Rho-kinase, Rho-associated kinase, Rho-associated protein kinase, PKA

Compound Identifiers

PubChem CID

56962369