GKI-1

SKU: orb1709606

Description

GKI-1 is a potent and selective inhibitor of Greatwall kinase (GWL), demonstrating IC₅₀ values of 4.9 µM and 2.5 µM against the full-length and kinase domain constructs, respectively. It exhibits stronger activity against ROCK1 (IC₅₀ = 11 µM) and weak inhibition of PKA. This tool compound is useful for studying cell cycle regulation, mitosis, and PP2A-B55 phosphatase signaling in cellular and biochemical assays.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2444764-03-6
• MW: 269.73
• Purity: 99.96% (May vary between batches)
• Formula: C₁₅H₁₂ClN₃
• SMILES: N(C=1C=C(C=CC1)C=2C=NNC2)C3=CC=C(Cl)C=C3
• Target: ROCK,Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (18.54 mM);DMSO:180 mg/mL (667.33 mM)

Bioactivity

• Target IC50:
  GWLFL (human):4.9 µM |GWLFL (human):4.9 µM|ROCK1:11 µM|GWL-KinDom (human):4.9 µM |GWL-KinDom (human):2.5 µM
• In Vitro:
  Treatment of HeLa cells with GKI-1 (25 and 50µM, 0-8.5 h) reduced ENSA/ARPP19 phosphorylation levels, resulting in reduced mitotic events, mitotic arrest/cell death, and cell division failure. GKI-1 inhibited full-length human GWL and showed cellular effects
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Greatwall (GWL), GKI-1, GKI 1, GKI1, hGWLFL, hGWL-KinDom

Compound Identifiers

PubChem CID

137333439