Ki16425

Catalog No.S1315

For research use only.

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.

Ki16425 Chemical Structure

CAS No. 355025-24-0

Selleck's Ki16425 has been cited by 19 publications

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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
chem1 cells Mn7hSpVv[3Srb36gZZN{[Xl? MV\BcpRi\2:waYP0JIFkfGm4aYT5JIF1KEySQUGg[ZhxemW|c3XkJIlvKGi3bXHuJINp\W1zIHPlcIx{KGG|c3Xzd4VlKGG|IHXm[oVkfCCxbjDpcpRz[WOnbHz1cIFzKGOjbHPpeY0hdW:kaXzpfoF1cW:wIHL5JGZNUVCUIHHzd4F6NCCLQ{WwQVAvODR4zszN M4nJVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMEW2OVQ5Lz5{MEC1OlU1QDxxYU6=
RH7777 NEXz[21HfW6ldHnvckBie3OjeR?= NEj4[oNDcW6maX7nJIFn\mmwaYT5JIZweiCOeYPvdIhwe3CqYYTp[IlkKGGlaXSgdoVk\XC2b4KgN{BmgHC{ZYPz[YQhcW5iUli3O|c4KHKjdDDo[ZBifG:vYTDj[YxteyxiS3m9NE4yPDkQvF2= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjB|M{K3NUc,OTZyM{OyO|E9N2F-
stellate cells MWTGeY5kfGmxbjDhd5NigQ>? NGfwbHdCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFzQRVEhemWlZYD0c5IhcW5icnH0JIhmeGG2aXOgd5RmdGyjdHWgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCueYPvdIhwe3CqYYTp[IlkKGGlaXStbY5lfWOnZDDpcpRz[WOnbHz1cIFzKGOjbHPpeY0hcW6obIX4MEBKSzVyPUCuNVbPxE1? NVPoRYxXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0Olc6QDZpPkG3OFY4QTh4PD;hQi=>
RH7777 MXnGeY5kfGmxbjDhd5NigQ>? Mn7hTY5pcWKrdHnvckBw\iCOUFGtbY5lfWOnZDDjZYxkcXWvIITyZY5{cWWwdIOgbY4hWkh5N{e3JJJifCCqZYDheI9u[SClZXzsd{BmgHC{ZYPzbY5oKEySQUOgdoVk\XC2b4KsJGlEPTB;MD6zNFHPxE1? MoC3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZyM{OyO|EoRjF4MEOzNlcyRC:jPh?=
RH7777 MnTBSpVv[3Srb36gZZN{[Xl? M{nwW2JqdmSrbnegZYZncW6rdImg[o9zKEy7c3;wbI9{eGijdHnkbYMh[WOrZDDy[YNmeHSxcjCxJIV5eHKnc4Pl[EBqdiCUSEe3O|chemG2IHjldIF1d22jIHPlcIx{NCCNaU2wMlQzPc7:TR?= M{DHdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MEOzNlcyLz5zNkCzN|I4OTxxYU6=
CHOK1 Ml:0SpVv[3Srb36gZZN{[Xl? M33acWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hemWlb33ibY5idnRiTGDBNUBz\WOncITvdkBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDsfZNweGixc4DoZZRq\GmlIHHjbYQucW6mdXPl[EBqdnS{YXPlcIx2dGG{IHPhcINqfW1iaX7mcJV5NCCLQ{WwQVAvPTIQvF2= NHi2e449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S2O|k5Pid-MUe0Olc6QDZ:L3G+
RH7777 MlPySpVv[3Srb36gZZN{[Xl? M4Xqe2lvcGmkaYTpc44hd2ZiTGDBMYlv\HWlZXSgZ4Ft[2m3bTD0doFve2mnboTzJIlvKFKKN{e3O{Bz[XRiaHXwZZRwdWFiY3XscJMh\XiycnXzd4lv\yCOUFGxJJJm[2WydH;yMEBKSzVyPUCuO|Yz|ryP NIPCbYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkCzN|I4OSd-MU[wN|MzPzF:L3G+
PC-3 NGnydmdHfW6ldHnvckBie3OjeR?= MUnCbY5lcW6pIHHm[olvcXS7IH\vdkBNgXOxcHjvd5Bp[XSrZHnjJIFkcWRicnXj[ZB1d3JiaX6gVGMuOyClZXzsd{whU2l;MT63OO69VQ>? NFXVZo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkCzN|I4OSd-MU[wN|MzPzF:L3G+
PC-3 MUHGeY5kfGmxbjDhd5NigQ>? NXjDbVl{UW6qaXLpeIlwdiCxZjDMVGEucW6mdXPl[EBk[WylaYXtJJRz[W6|aXXueJMhcW5iUFOtN{Bk\WyuczygTWM2OD1|LkO4OO69VQ>? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjB|M{K3NUc,OTZyM{OyO|E9N2F-
HEK293 NX3GTZg1TnWwY4Tpc44h[XO|YYm= M1jDb|YxKG2rboO= M{CxNWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hVFCDMjDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDBMYlv\HWlZXSgRXAuXEeILXHsdIhiKHKnbHXhd4UhfHKnYYTl[EA2KG2rboOgZoVnd3KnIFzQRUBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjC2NEBucW6| NHLnVog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1PFU2Pid-MkK2OVg2PTZ:L3G+
HEK293 NEj1UY5HfW6ldHnvckBie3OjeR?= Mn23OlAhdWmwcx?= MX3BcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGxRSTFicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEySQT3pcoR2[2WmIFHQMXRITi2jbIDoZUBz\WynYYPlJJRz\WG2ZXSgOUBucW6|IHLl[o9z\SCOUFGgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiNkCgcYlvew>? NXzG[GY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2OVg2PTZpPkKyOlU5PTV4PD;hQi=>
PC3 NWS0U4JQTnWwY4Tpc44h[XO|YYm= MXzBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEySQTDy[YNmeHSxcjDpckBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVGEucW6mdXPl[EBk\WyuIH3p[5JifGmxbh?= MnfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4NUi1OVYoRjJ{NkW4OVU3RC:jPh?=
CHO Mmq1SpVv[3Srb36gZZN{[Xl? MWfDc41x\XSrdHn2[UBidnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKEySQUGgdoVk\XC2b4Kgc5ZmemW6cILld5Nm\CCrbjDDTG8h[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVGEucW6mdXPl[EBcOzWVXVfUVIdidW2jUzDibY5lcW6pIHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF6MEizOkc,OjJzOEC4N|Y9N2F-
CHO NYLn[nhJTnWwY4Tpc44h[XO|YYm= NES4NFlEd22yZYTpeIl3\SCjboTh[49vcXO2IHHjeIl3cXS7IHH0JG4ufGW{bXnuZYwhO1iKQT30ZYdo\WRiaIXtZY4hVFCDMzDy[YNmeHSxcjDveoVz\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQRU1qdmS3Y3XkJHs{PVOfR2TQ[4FudWGVIHLpcoRqdmdiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> NUXkVYl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKxPFA5OzZpPkKyNVgxQDN4PD;hQi=>
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 Research:[4]
  • Animal Models: Male standard ddY-strain mice are used.
  • Dosages: 30 mg/kg.
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 474.96
Formula

C23H23ClN2O5S

CAS No. 355025-24-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NOC(=C1NC(=O)OC(C)C2=CC=CC=C2Cl)C3=CC=C(C=C3)CSCCC(=O)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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