JNJ-26854165 (Serdemetan)

For research use only. Not for use in humans.

Catalog No.S1172

7 publications

JNJ-26854165 (Serdemetan) Chemical Structure

Molecular Weight(MW): 328.41

JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

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Selleck's JNJ-26854165 (Serdemetan) has been cited by 7 publications

6 Customer Reviews

  • Mol Pharmacol 2014 85(3), 408-19. JNJ-26854165 (Serdemetan) purchased from Selleck.

    Sci Rep 2014 4, 4663. JNJ-26854165 (Serdemetan) purchased from Selleck.

  • Sci Rep 2014 4, 4663. JNJ-26854165 (Serdemetan) purchased from Selleck.

    Sci Rep 2014 4, 4663. JNJ-26854165 (Serdemetan) purchased from Selleck.

  • J Nat Med 2013 10.1007/s11418-014-0825-0. JNJ-26854165 (Serdemetan) purchased from Selleck.

    Curr Protoc Chem Biol 2013 5(3), 195-212. JNJ-26854165 (Serdemetan) purchased from Selleck.

Purity & Quality Control

Choose Selective p53 Inhibitors

Biological Activity

Description JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.
Targets
p53 [1]
(Cell-free assay)		 HDM2 [1]
(Cell-free assay)		 Mdm2 [2]
(Cell-free assay)
In vitro

JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. [1] JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. [2] A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KU-19-19 cell NEjMfmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLXTY5pcWKrdHnvckBw\iCqdX3hckBMXS1zOT2xPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQTN{M{[g{txO M2W0WXNCVkeHUh?=
H4 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPQ[nlKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOlcxPyEQvF2= NW\V[2xbW0GQR1XS
KGN cell NIfG[FhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF\udmFKdmirYnn0bY9vKG:oIHj1cYFvKEuJTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlIxPSEQvF2= NWXJSXZQW0GQR1XS
786-0 cell NF;1SmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXrQTmxsUW6qaXLpeIlwdiCxZjDoeY1idiB5OE[tNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzJ7OEmg{txO M{nvUXNCVkeHUh?=
769-P cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWS5UJNNUW6qaXLpeIlwdiCxZjDoeY1idiB5NkmtVEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDJ{MkSg{txO NHT5[|ZUSU6JRWK=
K5 cell NUnVPWxMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1r5XWlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkCxOlI1KM7:TR?= NIPtNIxUSU6JRWK=
MLMA cell M4Hyemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4Lne2lvcGmkaYTpc44hd2ZiaIXtZY4hU0:VQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xOzJzNzFOwG0> NYW5R|I3W0GQR1XS
MLMA cell M1XqbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfSTY5pcWKrdHnvckBw\iCqdX3hckBOVE2DIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6yPFcxOyEQvF2= NFjoXpVUSU6JRWK=
EW-7 cell M1rN[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWP6c2FGUW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4{OjZ7NTFOwG0> Mli0V2FPT0WU
SW1088 cell M2HoUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWXJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPFA3PTFizszN M{W3SnNCVkeHUh?=
MC-IXC cell NFrFUWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M36yfGlvcGmkaYTpc44hd2ZiaIXtZY4hVUNvSWjDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk45Pzd7MjFOwG0> NXu0SZZyW0GQR1XS
NCI-H2052 cell NGDxPZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV[yWWZTUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxPTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVU4KM7:TR?= MonKV2FPT0WU
IGR-1 cell NHfFZY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGlIWi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6xNlAzQCEQvF2= NH;jZmdUSU6JRWK=
DSH1 cell Moj6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1jGVGlvcGmkaYTpc44hd2ZiaIXtZY4hTFOKMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNlQzQTZizszN MmDsV2FPT0WU
PA-1 cell MlrCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1q0S2lvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuN|AxPToQvF2= MknLV2FPT0WU
SK-MEL-3 cell Mk\HS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX7KcYhPUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwM{GyNFch|ryP NF\DcGhUSU6JRWK=
SW900 cell MkjzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTByIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz60PFI2PSEQvF2= M{XDWHNCVkeHUh?=
CAKI-1 cell M{XpWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2SwS2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> NF;MdFZUSU6JRWK=
ES1 cell NFG1TnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIG2WWdKdmirYnn0bY9vKG:oIHj1cYFvKEWVMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVI5QTdizszN NWfmboxSW0GQR1XS
SK-N-DZ cell NX;UO2FVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvHOJVEUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3OMWRbKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy54MkW5OUDPxE1? NU\vS41qW0GQR1XS
RH-1 cell NHPUVnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvMcHBKdmirYnn0bY9vKG:oIHj1cYFvKFKKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY5PDZ|IN88US=> NXrtPZdpW0GQR1XS
ES8 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{fEPWlvcGmkaYTpc44hd2ZiaIXtZY4hTVN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz62PVcxOiEQvF2= MmjjV2FPT0WU
NEC8 cell M4nmU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXWTY5pcWKrdHnvckBw\iCqdX3hckBPTUN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63Olk5OiEQvF2= M3rEfHNCVkeHUh?=
LNCaP-Clone-FGC cell M1HNR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIDrbYdKdmirYnn0bY9vKG:oIHj1cYFvKEyQQ3HQMWNtd26nLV\HR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQDN3M{[g{txO NWHic4hDW0GQR1XS
HCE-4 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NE\vZYJKdmirYnn0bY9vKG:oIHj1cYFvKEiFRT20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46QDB5IN88US=> MYnTRW5ITVJ?
U-118-MG cell MlH0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoPPTY5pcWKrdHnvckBw\iCqdX3hckBWNTFzOD3NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODFyNk[g{txO M4XheXNCVkeHUh?=
GI-ME-N cell NHHyOZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF7X[XBKdmirYnn0bY9vKG:oIHj1cYFvKEeLLV3FMW4h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB6N{m2JO69VQ>? NWLibZprW0GQR1XS
LB1047-RCC cell MmLES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFyyR5RKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkG2NVQ{KM7:TR?= M1G0ZnNCVkeHUh?=
HT-1080 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPsTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4yQTl{MTFOwG0> NI\xSmFUSU6JRWK=
NB69 cell M3vzT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXH0c49GUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE4{PTB2NzFOwG0> NUXZNmZIW0GQR1XS
NCI-H1693 cell M4DYUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4DtSWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlk{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC52NEi5OUDPxE1? NHrlZmNUSU6JRWK=
HSC-3 cell MnXlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3XKNmlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlQ6QTN|IN88US=> Mk\kV2FPT0WU
MDA-MB-231 cell NEP0OGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIe3WYtKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk0zOzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12LkW1PFk6KM7:TR?= NX7OeGZpW0GQR1XS
HOS cell NIjoWIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4i2TWlvcGmkaYTpc44hd2ZiaIXtZY4hUE:VIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND63PFY{KM7:TR?= NVf0c25rW0GQR1XS
BT-549 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn;iTY5pcWKrdHnvckBw\iCqdX3hckBDXC13NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc5QDdizszN NH\LTGtUSU6JRWK=
NB17 cell NHjmZ4VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvRbFVFUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDl5NjFOwG0> MY\TRW5ITVJ?
5637 cell M1fhUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPuVGQ5UW6qaXLpeIlwdiCxZjDoeY1idiB3NkO3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QTZ3MjFOwG0> M3njcHNCVkeHUh?=
OVCAR-8 cell M4rWbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jsfmlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTJ2M{[g{txO MojmV2FPT0WU
G-402 cell NI[xTI5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2P3ZmlvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk{ODN3IN88US=> MnLaV2FPT0WU
BB30-HNC cell M4X0VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIKxeWRKdmirYnn0bY9vKG:oIHj1cYFvKEKEM{CtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5yN{KxPEDPxE1? MUHTRW5ITVJ?
HCC1806 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX7EZYhjUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxPFA3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5yOEOzPUDPxE1? NFzu[pVUSU6JRWK=
COLO-800 cell NUT3d5RHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnzSTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUiwNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOTJ4NDFOwG0> NYHke2Q{W0GQR1XS
FADU cell NWrjN5R[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn7mTY5pcWKrdHnvckBw\iCqdX3hckBHSUSXIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT6zOlU2PyEQvF2= NVL2UXJ[W0GQR1XS
NCI-H1651 cell NX;QeY5VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvKRmEyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkO5OFA6KM7:TR?= NEnsXZJUSU6JRWK=
AGS cell NHO4dIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXHJcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNEe3NVEh|ryP NF3GcWtUSU6JRWK=
CHP-212 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXrLV21CUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5|OUSwPUDPxE1? NVLYfWw3W0GQR1XS
YAPC cell MnPxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3nnfmlvcGmkaYTpc44hd2ZiaIXtZY4hYUGSQzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuOFc4OTFizszN M3rrZXNCVkeHUh?=
GOTO cell M1XGU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknwTY5pcWKrdHnvckBw\iCqdX3hckBIV1SRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60PVU4PiEQvF2= NYrocIJUW0GQR1XS
KYSE-510 cell NXvxdpFpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\mWWlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT21NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjVzMTFOwG0> MkjBV2FPT0WU
NCI-H2342 cell M{m5ZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHfNWWlKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlM1OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNUOyO|gh|ryP MoLLV2FPT0WU
BFTC-905 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU43Ojh|NTFOwG0> MnPiV2FPT0WU
EW-16 cell MoXJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVXs[nhvUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzJyOUOg{txO M1rGWXNCVkeHUh?=
SK-MEL-30 cell NIj6VJhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzR3NEOg{txO MWHTRW5ITVJ?
HLE cell NIPBRpNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFvDVnlKdmirYnn0bY9vKG:oIHj1cYFvKEiORTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuO|c1QDlizszN MXrTRW5ITVJ?
T98G cell NF:xSG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHQ6QEdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke5OlM2KM7:TR?= M1;BeHNCVkeHUh?=
HUTU-80 cell NXrTWm1UT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTNV5pKdmirYnn0bY9vKG:oIHj1cYFvKEiXVGWtPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njh2MkK4JO69VQ>? NIn6ZlRUSU6JRWK=
NOS-1 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUKxOVNOUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTR5Nk[g{txO MornV2FPT0WU
SW780 cell NHHafnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT65Olk1QSEQvF2= MWXTRW5ITVJ?
KYSE-180 cell M1jM[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvMUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46PzZ3NDFOwG0> NHXtbGRUSU6JRWK=
MDA-MB-361 cell M4S2XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUnJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njl6NkS3JO69VQ>? M4DYdXNCVkeHUh?=
SNU-C2B cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1jwSmlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLVOyRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvODFzM{ig{txO NGq4VFdUSU6JRWK=
NCI-H661 cell NH:zOG1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNk[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4xPjl2IN88US=> NWD6XlVSW0GQR1XS
OE33 cell NHHPWnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJG9GOzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG0N|g6KM7:TR?= NGTmVmNUSU6JRWK=
TYK-nu cell M3fYPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGDKcHVKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOjF6NkOg{txO MXnTRW5ITVJ?
COLO-792 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1TK[mlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjJ3MkG5JO69VQ>? MoHYV2FPT0WU
HEL cell MmfCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGT4enZKdmirYnn0bY9vKG:oIHj1cYFvKEiHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uNlY4PiEQvF2= MkfBV2FPT0WU
D-566MG cell NFXQd25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFrKZ3RKdmirYnn0bY9vKG:oIHj1cYFvKERvNU[2UWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjN|NEmxJO69VQ>? NHfBOoxUSU6JRWK=
U031 cell M3\oRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWHuTVJNUW6qaXLpeIlwdiCxZjDoeY1idiCXMEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok41OThzNjFOwG0> MoTBV2FPT0WU
COR-L23 cell NF7WVo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXGS49qUW6qaXLpeIlwdiCxZjDoeY1idiCFT2KtUFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi52M{O0OkDPxE1? NHfzclRUSU6JRWK=
NCI-H2452 cell NIfxbHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkS1NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPTJ{OEGg{txO NFn5fJhUSU6JRWK=
BB65-RCC cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIjHUGFKdmirYnn0bY9vKG:oIHj1cYFvKEKENkWtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi54NEW5JO69VQ>? NF:zO2FUSU6JRWK=
CAL-33 cell MnK3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mlj0TY5pcWKrdHnvckBw\iCqdX3hckBESUxvM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlY2PjZ3IN88US=> M4C0SXNCVkeHUh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p53 / HDM2 / HDMX / p21 / Noxa / Puma ; 

PubMed: 20736344     


OCI-AML-3 and MOLM-13 cells were incubated with a range of concentrations of JNJ-26854165 for 18 hours.

ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR ; 

PubMed: 23820125     


U266 and JeKo-1 cells were treated with JNJ-26854165 and cells harvested at the indicated time points.

MDM2 / p-MDM2 / p53 ; 

PubMed: 27999193     


K562 cells was harvested at 48 h after treatment with various JNJ-165 concentrations, and then nuclear and cytoplasmic extracts were prepared to check the levels of p53, MDM2 and p-MDM2 by Western blotting. Actin and LaminB were used as loading control respectively.

Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3 ; 

PubMed: 27999193     


CML cell lines were treated with JNJ-165 at the indicated doses for 48 h. Whole-cell lysates were extracted to assess the levels of BCR-ABL and phosphorylated (p)-BCR-ABL (Tyr177), and then were analyzed for BCR-ABL downstream signaling mediators p-CrkL (Try207), total Stat5, p-Stat5 (Tyr694), total Stat3, and p-Stat3 (Ser727) expression by Western blot analysis. The expression of β-actin was used as loading control. The data are representative of three determinations with identical results.

20736344 23820125 27999193
Growth inhibition assay
Cell viability; 

PubMed: 23820125     


MCL (B) and MM (C) cell lines were seeded in 96-well plates for viability analyses using WST-1 and treated with JNJ-26854165 for 72 hours. Results are expressed as the percentage of cell viability in relation to the vehicle-treated sample for each cell line, which was arbitrarily set at 100%

23820125
Immunofluorescence
p53; 

PubMed: 27999193     


Two-color fluorescence microscope analysis of antibody against p53 protein (green) and nuclei (DAPI staining, blue) showed nuclear accumulation of p53 in K562 cells with treatment of 1 μM JNJ-165, but not in control-treated cells after 48 h. Images were taken on a fluorescence microscopy (100×).

27999193
In vivo JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. [4]

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: OCI-AML-3, MOLM-13, NB4 and U937 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 72 hours
  • Method: Cell lines are maintained in RPMI 1640 medium containing 10% heat-inactivated fetal calf serum (FCS). OCI-AML-3, MOLM-13, NB4 and U937 cells are derived from acute myelogenous leukemia (AML) patients, K562 from a chronic myelogenous leukemia (CML) patient in blast crisis, and NALM-6, REH, P12-ICHIK
    (Only for Reference)
Animal Research:[4]
- Collapse
  • Animal Models: CB17SC scid-/- female mice.
  • Formulation: JNJ-26854165 is dissolved in DMSO and then diluted in water.
  • Dosages: ≤20 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (200.96 mM)
Ethanol 2 mg/mL (6.08 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
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 328.41
Formula

C21H20N4
CAS No. 881202-45-5
Storage powder
in solvent
Synonyms N/A
Smiles C(CC1=C[NH]C2=CC=CC=C12)NC3=CC=C(NC4=CC=NC=C4)C=C3

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID