Ki 16425
Chemical Name: 3-[[[4-[4-[[[1-(2-Chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]propanoic acid
Purity: ≥98%
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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.
Ohta et al.
Mol.Pharmacol., 2003;64:994 -
Lysophosphatidic acid (LPA) in malignant ascites stimulates motility of human pancreatic cancer cells through LPA1.
Yamada et al.
J.Biol.Chem., 2004;279:6595 -
Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling.
Yu et al.
Cell, 2012;150:780
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Citation for Ki 16425
The citations listed below are publications that use Tocris products. Selected citations for Ki 16425 include:
1 Citation: Showing 1 - 1
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Lysophosphatidic acid mediates myeloid differentiation within the human bone marrow microenvironment.
Authors: Evseenko Et al.
PLoS One 2013;8:e63718
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MG-63 cells were pre-incubated with 10 µM Ki 16425 for 30 min followed by treatment with 10 µM LPA for 3 h to follow COX-2 expression using Western blot. Ki 16425 inhibited COX-2 induction by LPA.
