G007-LK

SKU: orb1223323

Description

G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK displayed high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice. G007-LK was first discovered by Dr. Stefan Krauss's team.

Key Properties

• CAS Number: 1380672-07-0
• MW: 529.96
• Purity: >98% (HPLC)
• Formula: C₂₅H₁₆ClN₇O₃S
• SMILES: CS(=O)(=O)c1cnc(cc1)c1nnc(n1c1ccccc1Cl)/C=C/c1nnc(o1)c1ccc(cc1)C#N
• Target: AChR
• Solubility: DMSO : ≥ 30 mg/mL. 56.61 mM

Bioactivity

• In Vivo:
  G007-LK displays great pharmacokinetic profile in ICR mice. G007-LK (100 mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5+ intestinal stem cells in mice. G007-LK (100 mg/kg chow, p.o.) specifically targets LGR5+ WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2; R26R-tdTomato mice. G007-LK (10, 50 mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000 mg/kg chow, p. o) shows no effect on the alteration of duodenal morphology.
• In Vitro:
  G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively, and a cellular IC50 of 50 nM. G007-LK shows no inhibition of PARP1 at doses up to 20 μM, and has a high CYP3A4 inhibition IC50 value (>25 μM). G007-LK (0-20 μM) dose-dependently inhibits hepatocellular carcinoma (HCC) cell growth. G007-LK also downregulates the levels of YAP by upregulating AMOTL1 and AMOTL2 in HCC cell lines. In addition, G007-LK (0-20 μM) synergizes with MEK and AKT inhibitors to suppress HCC cell proliferation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

G007LK | G007LK | G007 LK

Quick Database Links

Gene Symbol

AChR