Ki16198

Catalog No.S2906 Batch:S290601

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Technical Data

Formula

C24H25ClN2O5S
Molecular Weight 488.98 CAS No. 355025-13-7
Solubility (25°C)* In vitro DMSO 98 mg/mL (200.41 mM)
Ethanol 35 mg/mL (71.57 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 Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.
Targets
LPA1 [1] LPA3 [1]
0.34 μM(Ki) 0.93 μM(Ki)
In vitro Ki16198 or Ki16425 substantially inhibits LPA1- and LPA3-mediated responses with a similar potency, with low potency to LPA2 and no activity to LPA4, LPA5 and LPA6. Ki16198 (10 μM) is also effective to inhibit migration and invasion responses to LPA in YAPC-PD cancer cell line with a potency similar to that of Ki16425. Ki16198 (10 μM) inhibits the LPA-induced expression of proMMP-9 protein and mRNA in YAPC-PD cells. [1] Ki16198 (1 μM) inhibits the proliferation of lpa1Δ-1 and lpa1Δ+-1 cells by about 70%. [2]
In vivo Ki16198 (2 mg/kg) significantly decreases the total metastatic node weight in the peritoneal cavity and ascites formation by 50% in YAPC-PD xenograft mouse model. [1] Ki16198 (60 mg/kg orally) significantly inhibits lactate-induced limb lesions in rats. [3]

Protocol (from reference)

Kinase Assay:[1]
  • Inositolphosphate response

    RH7777 cells expressing LPA1, LPA2, LPA3, LPA4, or LPA5 are cultured on collagen-coated 12-well dishes in the growth medium, and then the medium is changed to TCM199 containing 2 μCi/mL [3H]inositol and 0.1% (w/v) BSA (fraction V). After 24 h later, the cells are washed three times with HEPES-buffered medium, which consisted of 20 mM Hepes (pH 7.4), 134 mM NaCl, 4.7 mM KCl, 1.2 mM KH2PO4, 1.2 mM MgSO4, 2 mM CaCl2, 2.5 mM NaHCO3, 5 mM glucose, and 0.1% (w/v) BSA, and incubated for 30 min with the indicated concentrations of Ki16425 or Ki16198 with or without 1 μM LPA in the presence of 10 mM LiCl in the same medium at final volume of 0.5 mL. The reaction is terminated by adding 1 N HCl (0.1 mL) and freezing the cells. The supernatant (acid extract in 0.5 mL) of the thawed cells is used for the separation of [3H]inositol phosphate fractions. The results are normalized to 105 dpm of the total radioactivity incorporated into the cellular inositol lipids. The radioactivity of the trichloroacetic acid (5%)-insoluble fraction is measured as the total radioactivity.
Cell Assay:[1]
  • Cell lines

    YAPC-PD cells or Panc-1 cells

  • Concentrations

    10 μM

  • Incubation Time

    24 hours

  • Method

    YAPC-PD cells or Panc-1 cells are seeded on 12-well plates at 1 × 104 cells in 1 mL. Sixteen hours before experiments, the medium is changed to RPMI1640 containing 0.1% BSA. Then, the cells are stimulated for 24 h in the same medium in the presence or absence of Ki16198. The proliferation activity is measured by the cellular ability to reduce MTT (3-(4,5-Dimethyl-2-thiazoyl)-2,5-diphenyltetrazolium bromide
Animal Study:[1]
  • Animal Models

    YAPC-PD xenograft mouse model

  • Dosages

    2 mg/kg

  • Administration

    Orally

Customer Product Validation

Data from [Data independently produced by , , Neurosci Bull, 2016, 32(5):445-54.]

Selleck's Ki16198 has been cited by 1 publication

Modulation of Nav1.8 by Lysophosphatidic Acid in the Induction of Bone Cancer Pain [Pan HL, et al. Neurosci Bull, 2016, 32(5):445-54] PubMed: 27631681

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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.