Biological Activity
Antagonist of the lysophosphatidic acid receptors LPA1 and LPA3 (Ki values are 0.25 and 0.36 μM respectively, in a GTPγS binding assay). Blocks LPA-induced dephosphorylation of Yes-associated protein (YAP) and WW domain-containing transcription regulator protein 1 (TAZ), inhibiting the Hippo signaling pathway, in HEK293A cells.
Technical Data
M. Wt | 474.96 |
Formula | C23H23ClN2O5S |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 355025-24-0 |
PubChem ID | 10367662 |
InChI Key | LLIFMNUXGDHTRO-UHFFFAOYSA-N |
Smiles | CC1=NOC(C2=CC=C(CSCCC(O)=O)C=C2)=C1NC(OC(C3=CC=CC=C3Cl)C)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
1eq. NaOH | 9.5 | 20 | |
DMSO | 47.5 | 100 | |
ethanol | 47.5 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 474.96. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.11 mL | 10.53 mL | 21.05 mL |
5 mM | 0.42 mL | 2.11 mL | 4.21 mL |
10 mM | 0.21 mL | 1.05 mL | 2.11 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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References
References are publications that support the products' biological activity.
Ohta et al (2003) Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol.Pharmacol. 64 994 PMID: 14500756
Yamada et al (2004) Lysophosphatidic acid (LPA) in malignant ascites stimulates motility of human pancreatic cancer cells through LPA1. J.Biol.Chem. 279 6595 PMID: 14660630
Yu et al (2012) Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell 150 780 PMID: 22863277
Keywords: Ki 16425, supplier, Ki16425, lysophosphatidic, acid, receptors, LPA1, LPA2, LPA3, YAP, TAZ, HIPPO, Lysophosphatidic, Acid, Receptors, Lysophosphatidic, Acid, Receptors, Tocris Bioscience