Ki16425

Catalog No.S1315

Ki16425 Chemical Structure

Molecular Weight(MW): 474.96

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.

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Cited by 8 Publications

4 Customer Reviews

  • Ethanol intake and preference in male mice treated with Ki16425 during 24 h. Ethanol intake (A) and ethanol preference (B) in wild-type mice treated with vehicle or Ki16425 (5 and 20 mg/kg, i.p.).

    Neuropharmacology, 2016, 103:92-103. Ki16425 purchased from Selleck.

    J Cell Mol Med 2014 18(1), 156-69. Ki16425 purchased from Selleck.

  • LPA treatment (2 uM) for 2 h in the presence of Ki16425 (10 uM, n = 40) results in a 40% decrease in FN-integrin adhesion compared with the cells treated with LPA alone (n = 40).

    Front Physiol 2014 5, 413. Ki16425 purchased from Selleck.

    MC3T3-E1 cells were treated with or without Ki16425 (20 μM; a specific inhibitor of LPA1/3) for 30 min were subsequently stimulated with LPA for 2 h; the CCN2 mRNA expression levels were measured by RT-qPCR. **P<0.01

    Int J Mol Med, 2016, 37(2):468-74. Ki16425 purchased from Selleck.

Purity & Quality Control

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human chem1 cells NHvJfVhHfW6ldHnvckBie3OjeR?= M1nwT2FvfGGpb37pd5Qh[WO2aY\peJkh[XRiTGDBNUBmgHC{ZYPz[YQhcW5iaIXtZY4h[2inbUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJIlvfHKjY3XscJVt[XJiY3HsZ4l2dSCvb3LpcIl7[XSrb36gZpkhTkyLUGKgZZN{[XluIFnDOVA:OC5yNE[g{txO NH3tbVAzODB3NkW0PC=>
RH7777 rat hepatoma cells M13yXWZ2dmO2aX;uJIF{e2G7 Mlf5Rolv\GmwZzDh[oZqdmm2eTDmc5IhVHm|b4Doc5NxcGG2aXTpZ{Bi[2mmIILlZ4VxfG:{IEOg[ZhxemW|c3XkJIlvKFKKN{e3O{Bz[XRiaHXwZZRwdWFiY3XscJMtKEurPUCuNVQ5KM7:TR?= MnvlNVYxOzN{N{G=
rat hepatic stellate cells NEj5N|RHfW6ldHnvckBie3OjeR?= MULBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEySQUGgdoVk\XC2b4KgbY4hemG2IHjldIF1cWNic4TlcIxifGViY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBtgXOxcHjvd5Bp[XSrZHnjJIFkcWRvaX7keYNm\CCrboTyZYNmdGy3bHHyJINidGOrdX2gbY5ndHW6LDDJR|UxRTBwMU[g{txO NXzFboltOTd2Nke5PFY>
RH7777 rat hepatoma cells NGj6ZY5HfW6ldHnvckBie3OjeR?= M17jW2lvcGmkaYTpc44hd2ZiTGDBMYlv\HWlZXSgZ4Ft[2m3bTD0doFve2mnboTzJIlvKFKKN{e3O{Bz[XRiaHXwZZRwdWFiY3XscJMh\XiycnXzd4lv\yCOUFGzJJJm[2WydH;yMEBKSzVyPUCuN|AyKM7:TR?= MX[xOlA{OzJ5MR?=
CHOK1 cells M3voRWZ2dmO2aX;uJIF{e2G7 MojDRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBz\WOxbXLpcoFvfCCOUFGxJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFSF;LNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHz5d49xcG:|cHjheIllcWNiYXPp[E1qdmS3Y3XkJIlvfHKjY3XscJVt[XJiY3HsZ4l2dSCrbn\seZgtKEmFNUC9NE42OSEQvF2= NF3pUZIyPzR4N{m4Oi=>
PC-3 cells MnT1SpVv[3Srb36gZZN{[Xl? MX7CbY5lcW6pIHHm[olvcXS7IH\vdkBNgXOxcHjvd5Bp[XSrZHnjJIFkcWRicnXj[ZB1d3JiaX6gVGMuOyClZXzsd{whU2l;MT63OEDPxE1? NF3HOYMyPjB|M{K3NS=>
HEK293 cells M2DVemZ2dmO2aX;uJIF{e2G7 M4PVflUhdWmwcx?= M3;UXmFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hVFCDMTDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDBMYlv\HWlZXSgRXAuXEeILXHsdIhiKHKnbHXhd4UhfHKnYYTl[EA2KG2rboOgZoVnd3KnIFzQRUBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjC2NEBucW6| NGLKdFQzOjZ3OEW1Oi=>

... Click to View More Cell Line Experimental Data

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

Animal Research:[4]
+ Expand
  • Animal Models: Male standard ddY-strain mice are used.
  • Formulation: Dissolved in sesame oil just before administration.
  • Dosages: 30 mg/kg.
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (197.91 mM)
Ethanol 94 mg/mL (197.91 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+95% Corn oil
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 474.96
Formula

C23H23ClN2O5S

CAS No. 355025-24-0
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID