Ki16425

Catalog No.S1315 Batch:S131504

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Technical Data

Formula

C23H23ClN2O5S
Molecular Weight 474.96 CAS No. 355025-24-0
Solubility (25°C)* In vitro DMSO 94 mg/mL (197.91 mM)
Ethanol 94 mg/mL (197.91 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6.
Targets
LPA1 [1]
(RH7777 cells)		 LPA3 [1]
(RH7777 cells)		 LPA2 [1]
(RH7777 cells)
0.34 μM(Ki) 0.93 μM(Ki) 6.5 μM(Ki)
In vitro Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only a marginal effect in PC-12 cells and HL-60 cells, which means that Ki16425 seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. Ki16425 inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts. [1] Ki16425 reduces the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Ki16425 also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells. [2] Ki16425 markedly inhibits the expressions of COX-2 protein induced by synovial fluids. The enhancement of the IL-1 action by LPA on COX-2 expression is also inhibited by Ki16425. [3]
In vivo Ki-16425 (30 mg/kg, i.p.) completely blocks LPA-induced neuropathic pain-like behaviors, when administered 30 min but not 90 min before lysophosphatidic acid injection, suggesting that Ki-16425 is a short-lived inhibitor. Ki-16425 also inhibits nerve injury-induced up-regulation of Caα2δ-1 in the dorsal root ganglion and reduction of SP immunoreactivity in the spinal dorsal horn. [4]

Protocol (from reference)

Animal Study:[4]
  • Animal Models

    Male standard ddY-strain mice are used.

  • Dosages

    30 mg/kg.

  • Administration

    Administered via i.p.

Customer Product Validation

Data from [J Cell Mol Med, 2014, 18(1), 156-69]

Data from [Data independently produced by Front Physiol, 2014, 5, 413]

Data from [Data independently produced by , , Neuropharmacology, 2016, 103:92-103]

Data from [Data independently produced by , , Int J Mol Med, 2016, 37(2):468-74]

Selleck's Ki16425 has been cited by 24 publications

Lysophosphatidic acid is associated with oocyte maturation by enhancing autophagy via PI3K-AKT-mTOR signaling pathway in granulosa cells [ J Ovarian Res, 2023, 16(1):137] PubMed: 37434211
Lysophosphatidic acid is associated with oocyte maturation by enhancing autophagy via PI3K-AKT-mTOR signaling pathway in granulosa cells [ J Ovarian Res, 2023, 16(1):137] PubMed: 37434211
Recapitulating early human development with 8C-like cells [ Cell Rep, 2022, 39(12):110994] PubMed: 35732112
Lysophosphatidic acid suppresses apoptosis of high-grade serous ovarian cancer cells by inducing autophagy activity and promotes cell-cycle progression via EGFR-PI3K/Aurora-AThr288-geminin dual signaling pathways [ Front Pharmacol, 2022, 13:1046269] PubMed: 36601056
LPA signaling acts as a cell-extrinsic mechanism to initiate cilia disassembly and promote neurogenesis [ Nat Commun, 2021, 12(1):662] PubMed: 33510165
Lysophosphatidic Acid-Induced EGFR Transactivation Promotes Gastric Cancer Cell DNA Replication by Stabilizing Geminin in the S Phase [ Front Pharmacol, 2021, 12:706240] PubMed: 34658851
LPA receptor1 antagonists as anticancer agents suppress human lung tumours. [ Eur J Pharmacol, 2020, 868:172886] PubMed: 31866407
Lysophosphatidic acid guides the homing of transplanted olfactory ensheathing cells to the lesion site after spinal cord injury in rats. [ Exp Cell Res, 2019, 379(1):65-72] PubMed: 30898547
Lysophosphatidic acid induces ligamentum flavum hypertrophy through the LPAR1/Akt pathway [ Cellular Physiology and Biochemistry, 2018, 45 (4): 1472–1486.] PubMed: None
Lysophosphatidic Acid Induces Ligamentum Flavum Hypertrophy Through the LPAR1/Akt Pathway [ Cell Physiol Biochem, 2018, 45(4):1472-1486] PubMed: 29466791

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.