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Submit ReviewKi 16425
说明： LPA1 and LPA3 receptor antagonist
化学名： 3-[[[4-[4-[[[1-(2-Chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]phenyl]methyl]thio]propanoic acid
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for Ki 16425
| 分子量 | 474.96 |
| 公式 | C23H23ClN2O5S |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Ki 16425
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 47.5 | 100 | |
| 1eq. NaOH | 9.5 | 20 |
制备储备液 for Ki 16425
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Ki 16425
参考文献 for Ki 16425
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 Ki 16425 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Ki 16425 的部分引用包括：
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
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Ki 16425 inhibits LPA-mediated COX-2 activation.
By
Anonymous on 12/13/2018
分析类型： In Vitro
种属： Human
细胞系/组织： 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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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.