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Submit ReviewKi 16425
Description: LPA1 and LPA3 receptor antagonist
Chemical Name: 3-[[[4-[4-[[[1-(2-Chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]propanoic acid
Purity: ≥98% (HPLC)
Biological Activity for Ki 16425
Ki 16425 is an 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 for Ki 16425
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ki 16425
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.5 | 100 | |
| 1eq. NaOH | 9.5 | 20 |
Preparing Stock Solutions for Ki 16425
The following data is based on the product molecular weight 474.96. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for Ki 16425
References for Ki 16425
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Ki 16425, please let us know.
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Keywords: Ki 16425, Ki 16425 supplier, Ki16425, lysophosphatidic, acid, receptors, LPA1, LPA2, LPA3, YAP, TAZ, HIPPO, Lysophosphatidic, Acid, Receptors, Hippo/Yap, signaling, 5056, Tocris Bioscience
2 Citations for Ki 16425
Citations are publications that use Tocris products. Selected citations for Ki 16425 include:
Jinsong et al (2019) Ovarian cancer cell-derived lysophosphatidic acid induces glycolytic shift and cancer-associated fibroblast-phenotype in normal and peritumoral fibroblasts. Cancer Lett 442 464-474 PMID: 30503552
Evseenko et al (2013) Lysophosphatidic acid mediates myeloid differentiation within the human bone marrow microenvironment. PLoS One 8 e63718 PMID: 23696850
Do you know of a great paper that uses Ki 16425 from Tocris? Please let us know.
Reviews for Ki 16425
Average Rating: 5 (Based on 1 Review.)
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Ki 16425 inhibits LPA-mediated COX-2 activation.
By
Anonymous on 12/13/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma
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.
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