JNJ-26854165 (Serdemetan)

Catalog No.S1172

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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In DMSO USD 140 In stock
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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 MkH6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIDoO4dKdmirYnn0bY9vKG:oIHj1cYFvKEuXLUG5MVE6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC57M{KzOkDPxE1? Mm\iV2FPT0WU
H4 cell M3;XZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYrzWlhUUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFY4ODdizszN NET0WIdUSU6JRWK=
KGN cell MoOwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV:2fYNjUW6qaXLpeIlwdiCxZjDoeY1idiCNR16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlYzODVizszN NGjRZWlUSU6JRWK=
786-0 cell NYnCSZRWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGG1WYhKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ojl6OTFOwG0> NWmxSY1VW0GQR1XS
769-P cell M1;P[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HqXmlvcGmkaYTpc44hd2ZiaIXtZY4hPzZ7LWCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlgzOjJ2IN88US=> M4\GVnNCVkeHUh?=
K5 cell MnTsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrjTY5pcWKrdHnvckBw\iCqdX3hckBMPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMEG2NlQh|ryP M3f3UnNCVkeHUh?=
MLMA cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn;NTY5pcWKrdHnvckBw\iCqdX3hckBMV1OFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA{OjF5IN88US=> MWnTRW5ITVJ?
MLMA cell NX;BUZB[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG1NVUFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkK4O|A{KM7:TR?= Mkf3V2FPT0WU
EW-7 cell NGqzZVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGVYNTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkOyOlk2KM7:TR?= M{DHc3NCVkeHUh?=
SW1088 cell NH3meFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWHncnNQUW6qaXLpeIlwdiCxZjDoeY1idiCVV{GwPFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjhyNkWxJO69VQ>? M{\RZ3NCVkeHUh?=
MC-IXC cell NVPVVVVmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;IeWlvcGmkaYTpc44hd2ZiaIXtZY4hVUNvSWjDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk45Pzd7MjFOwG0> MkG1V2FPT0WU
NCI-H2052 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXmwZXdUUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxPTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkC4NVU4KM7:TR?= MluxV2FPT0WU
IGR-1 cell NH\ud5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVfsOJFuUW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOTJyMkig{txO MnrzV2FPT0WU
DSH1 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmD5TY5pcWKrdHnvckBw\iCqdX3hckBFW0hzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6yOFI6PiEQvF2= M{LtTXNCVkeHUh?=
PA-1 cell NFrzO2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoHETY5pcWKrdHnvckBw\iCqdX3hckBRSS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6zNFA2Qc7:TR?= NW\5VGlMW0GQR1XS
SK-MEL-3 cell MmX3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml;LTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOzF{MEeg{txO NGG5U3JUSU6JRWK=
SW900 cell NYfkNGJLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2XRZWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7MECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ5OjV3IN88US=> NFOxdIVUSU6JRWK=
CAKI-1 cell NVLYNYRvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;YNGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GNST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42Ojd|ODFOwG0> M4HJeXNCVkeHUh?=
ES1 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXT3N3R{UW6qaXLpeIlwdiCxZjDoeY1idiCHU{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlUzQDl5IN88US=> M{n1[XNCVkeHUh?=
SK-N-DZ cell NIrle2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvoTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVTaJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{43OjV7NTFOwG0> NIfxZ4FUSU6JRWK=
RH-1 cell M3HOS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFWx[2lKdmirYnn0bY9vKG:oIHj1cYFvKFKKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY5PDZ|IN88US=> MYTTRW5ITVJ?
ES8 cell M3Gxe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNkm3NFIh|ryP MkTMV2FPT0WU
NEC8 cell MnzhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XWc2lvcGmkaYTpc44hd2ZiaIXtZY4hVkWFODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuO|Y6QDJizszN MnTIV2FPT0WU
LNCaP-Clone-FGC cell NH7NOotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mo\ITY5pcWKrdHnvckBw\iCqdX3hckBNVkOjUD3DcI9v\S2IR1OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlg{PTN4IN88US=> NX;RUVdlW0GQR1XS
HCE-4 cell NVq3ZVF6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEP3WpdKdmirYnn0bY9vKG:oIHj1cYFvKEiFRT20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46QDB5IN88US=> NYDiZ|VZW0GQR1XS
U-118-MG cell NV\1TZRUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF3RbIZKdmirYnn0bY9vKG:oIHj1cYFvKFVvMUG4MW1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5yMUC2OkDPxE1? NXrzcYV2W0GQR1XS
GI-ME-N cell M{TqUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3PYeWlvcGmkaYTpc44hd2ZiaIXtZY4hT0lvTVWtUkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvODh5OU[g{txO MWPTRW5ITVJ?
LB1047-RCC cell Mn2xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUS1ZY5lUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6xOlE1OyEQvF2= NVnJVY5mW0GQR1XS
HT-1080 cell M2jTN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE6QTJzIN88US=> M3zDb3NCVkeHUh?=
NB69 cell MnP4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;ScWlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuN|UxPDdizszN M2\ybXNCVkeHUh?=
NCI-H1693 cell NH61XZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rWXmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlk{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC52NEi5OUDPxE1? NU\uN|BEW0GQR1XS
HSC-3 cell M3HpUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlnrTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuOFk6OzNizszN NE[2OW5USU6JRWK=
MDA-MB-231 cell NVf6T4VvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rQUmlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNUW4PVkh|ryP NXywZWhDW0GQR1XS
HOS cell MmjvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\ITY5pcWKrdHnvckBw\iCqdX3hckBJV1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke4OlMh|ryP Ml7iV2FPT0WU
BT-549 cell NYXHRlZsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3npV2lvcGmkaYTpc44hd2ZiaIXtZY4hSlRvNUS5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE44QDh5IN88US=> MmLYV2FPT0WU
NB17 cell NFnaWZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYDJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke4PVc3KM7:TR?= MW\TRW5ITVJ?
5637 cell MoPFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJFU3OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke5OlUzKM7:TR?= M4PxZXNCVkeHUh?=
OVCAR-8 cell M3L3cmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2njVmlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTJ2M{[g{txO M4nWZ3NCVkeHUh?=
G-402 cell M4foTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGDETFBKdmirYnn0bY9vKG:oIHj1cYFvKEdvNECyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE46OzB|NTFOwG0> NXvRZ5E1W0GQR1XS
BB30-HNC cell MoHpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHX5Z2NKdmirYnn0bY9vKG:oIHj1cYFvKEKEM{CtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5yN{KxPEDPxE1? MYjTRW5ITVJ?
HCC1806 cell MoT0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXrjTIlLUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxPFA3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5yOEOzPUDPxE1? M{jJUXNCVkeHUh?=
COLO-800 cell NGnIVnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzSTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUiwNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOTJ4NDFOwG0> M3S1OnNCVkeHUh?=
FADU cell NVr0[lU2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1nG[GlvcGmkaYTpc44hd2ZiaIXtZY4hTkGGVTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuN|Y2PTdizszN MknsV2FPT0WU
NCI-H1651 cell M2jFWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEDaU2xKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwM{m0NFkh|ryP NW\4eFc4W0GQR1XS
AGS cell M3fSemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwNEe3NVEh|ryP NUTzNIRPW0GQR1XS
CHP-212 cell NVLQW2I3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGNJWC1{MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM6PDB7IN88US=> Ml3jV2FPT0WU
YAPC cell MkDFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3flW2lvcGmkaYTpc44hd2ZiaIXtZY4hYUGSQzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuOFc4OTFizszN Mo\hV2FPT0WU
GOTO cell NIrMVIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLpeot[UW6qaXLpeIlwdiCxZjDoeY1idiCJT2TPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41QTV5NjFOwG0> NF7sUXBUSU6JRWK=
KYSE-510 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4fLcGlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT21NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjVzMTFOwG0> M2KzfnNCVkeHUh?=
NCI-H2342 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4rPfWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS53M{K3PEDPxE1? M37uO3NCVkeHUh?=
BFTC-905 cell M2f1fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nkWWlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjZ{OEO1JO69VQ>? NEPVdllUSU6JRWK=
EW-16 cell M2fyfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PqVmlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlczODl|IN88US=> Mkj4V2FPT0WU
SK-MEL-30 cell M{fxO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGLhVpdKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{S1OFMh|ryP MmTzV2FPT0WU
HLE cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV;ySZhGUW6qaXLpeIlwdiCxZjDoeY1idiCKTFWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc4PDh7IN88US=> Mn\ZV2FPT0WU
T98G cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF;td5ZKdmirYnn0bY9vKG:oIHj1cYFvKFR7OFegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlc6PjN3IN88US=> MnewV2FPT0WU
HUTU-80 cell NGS2[Y5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1zHR2lvcGmkaYTpc44hd2ZiaIXtZY4hUFWWVT24NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDR{Mkig{txO NIK5T4dUSU6JRWK=
NOS-1 cell Mn;VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{jqTmlvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlk1PzZ4IN88US=> NUTlNZlbW0GQR1XS
SW780 cell NEnlOlVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXflfW0xUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQTZ7NEmg{txO MmTEV2FPT0WU
KYSE-180 cell NInhdXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFrPUYFKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNVgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS57N{[1OEDPxE1? MUnTRW5ITVJ?
MDA-MB-361 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVHhWGVYUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT65PFY1PyEQvF2= M{[3Z3NCVkeHUh?=
SNU-C2B cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3Wxc2lvcGmkaYTpc44hd2ZiaIXtZY4hW06XLVOyRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvODFzM{ig{txO NFG5OWRUSU6JRWK=
NCI-H661 cell NXHOd5pjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHXxO4RKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlYyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5yNkm0JO69VQ>? M3vadHNCVkeHUh?=
OE33 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF:xWYVKdmirYnn0bY9vKG:oIHj1cYFvKE:HM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlE1Ozh7IN88US=> MVvTRW5ITVJ?
TYK-nu cell NF[wUZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{nLd2lvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zOTh4MzFOwG0> NGTNeYdUSU6JRWK=
COLO-792 cell NXziTWh5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vN{myJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4zPTJzOTFOwG0> NEHIZ5RUSU6JRWK=
HEL cell MkC4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHJTY5pcWKrdHnvckBw\iCqdX3hckBJTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkK2O|Yh|ryP NHrFfXdUSU6JRWK=
D-566MG cell M1vEeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWfNUnJbUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi5|M{S5NUDPxE1? NFTVR2pUSU6JRWK=
U031 cell M4DOW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIKyXnRKdmirYnn0bY9vKG:oIHj1cYFvKFVyM{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQyQDF4IN88US=> M3rveXNCVkeHUh?=
COR-L23 cell NHvFRmtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{TOS2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:ULVyyN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPDN|NE[g{txO NW\oOG1rW0GQR1XS
NCI-H2452 cell M{D2[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkS1NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPTJ{OEGg{txO Mmq2V2FPT0WU
BB65-RCC cell NVWzUnRsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17Kb2lvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjZ2NUmg{txO M2HlUnNCVkeHUh?=
CAL-33 cell NHHNO5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnSwTY5pcWKrdHnvckBw\iCqdX3hckBESUxvM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlY2PjZ3IN88US=> NXHROXRGW0GQR1XS

... 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

Bio Calculators

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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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.

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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID