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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USD 370 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 M33GNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHydJBzUW6qaXLpeIlwdiCxZjDoeY1idiCNVT2xPU0yQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOUOyN|Yh|ryP M1PiVXNCVkeHUh?=
H4 cell Mo\yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yNkewO{DPxE1? NEn6eFNUSU6JRWK=
KGN cell NFe4cG1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnPJTY5pcWKrdHnvckBw\iCqdX3hckBMT05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLk[yNFUh|ryP NGrpO3dUSU6JRWK=
786-0 cell NFW5VpJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlk5QSEQvF2= MXnTRW5ITVJ?
769-P cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkGxTY5pcWKrdHnvckBw\iCqdX3hckA4PjlvUDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuPFIzOjRizszN MV3TRW5ITVJ?
K5 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5yMU[yOEDPxE1? NV3wepRSW0GQR1XS
MLMA cell NF\WeVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn:xTY5pcWKrdHnvckBw\iCqdX3hckBMV1OFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA{OjF5IN88US=> NXTIfnREW0GQR1XS
MLMA cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYr3SWlFUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4zQDdyMzFOwG0> Ml24V2FPT0WU
EW-7 cell NWLsdVNbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzhTY5pcWKrdHnvckBw\iCqdX3hckBGXy15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6zNlY6PSEQvF2= Mn3vV2FPT0WU
SW1088 cell NHrU[G9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuPFA3PTFizszN NV\4dnNlW0GQR1XS
MC-IXC cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFrpRVVKdmirYnn0bY9vKG:oIHj1cYFvKE2FLVnYR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQDd5OUKg{txO M4DVPHNCVkeHUh?=
NCI-H2052 cell NFjRXo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4P3[GlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFUzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5yOEG1O{DPxE1? M4PqVHNCVkeHUh?=
IGR-1 cell M4f2e2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{Dj[mlvcGmkaYTpc44hd2ZiaIXtZY4hUUeULUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlEzODJ6IN88US=> NGjzUndUSU6JRWK=
DSH1 cell Mn6wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGRUUDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkK0Nlk3KM7:TR?= NUTMRpd2W0GQR1XS
PA-1 cell NYTUOol7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXXJcohq[mm2aX;uJI9nKGi3bXHuJHBCNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkOwNFU6|ryP NH;we2lUSU6JRWK=
SK-MEL-3 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rXcGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjNzMkC3JO69VQ>? NIDNO2xUSU6JRWK=
SW900 cell M3q5Nmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF\mSpBKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUCwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41QDJ3NTFOwG0> NF:xRopUSU6JRWK=
CAKI-1 cell MlLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MojSTY5pcWKrdHnvckBw\iCqdX3hckBESUuLLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlUzPzN6IN88US=> MWnTRW5ITVJ?
ES1 cell Mlr1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHoU29KdmirYnn0bY9vKG:oIHj1cYFvKEWVMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOVI5QTdizszN NHPYWmdUSU6JRWK=
SK-N-DZ cell M3XEV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LZSGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTj3EXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPjJ3OUWg{txO MmTUV2FPT0WU
RH-1 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPVTY5pcWKrdHnvckBw\iCqdX3hckBTUC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz62PFQ3OyEQvF2= MnHVV2FPT0WU
ES8 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGVUQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNkm3NFIh|ryP MnHwV2FPT0WU
NEC8 cell M1PnbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmLyTY5pcWKrdHnvckBw\iCqdX3hckBPTUN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz63Olk5OiEQvF2= MVHTRW5ITVJ?
LNCaP-Clone-FGC cell Ml;sS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1S1OGlvcGmkaYTpc44hd2ZiaIXtZY4hVE6FYWCtR4xwdmVvRlfDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{45OzV|NjFOwG0> NYrUNJFoW0GQR1XS
HCE-4 cell MljwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fJW2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOHLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk5ODdizszN M4rFZXNCVkeHUh?=
U-118-MG cell Mm\6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWPrO5d1UW6qaXLpeIlwdiCxZjDoeY1idiCXLUGxPE1OTyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwMEGwOlYh|ryP M4[4d3NCVkeHUh?=
GI-ME-N cell NUH1dHFsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjlUIpKdmirYnn0bY9vKG:oIHj1cYFvKEeLLV3FMW4h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjB6N{m2JO69VQ>? NU\WZlFIW0GQR1XS
LB1047-RCC cell M{HtNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWTIWnQyUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6xOlE1OyEQvF2= NIiwXJpUSU6JRWK=
HT-1080 cell M{Hpbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYPJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTFyOECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20MlE6QTJzIN88US=> NEPlRpFUSU6JRWK=
NB69 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mni5TY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND6zOVA1PyEQvF2= MlXzV2FPT0WU
NCI-H1693 cell NF\kUlFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4\ISWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlk{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC52NEi5OUDPxE1? Mnf5V2FPT0WU
HSC-3 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\zTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuOFk6OzNizszN M{LYU3NCVkeHUh?=
MDA-MB-231 cell NWnUNGtJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjV3OEm5JO69VQ>? NYfmUGx6W0GQR1XS
HOS cell NUjSXG9yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{LX[WlvcGmkaYTpc44hd2ZiaIXtZY4hUE:VIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND63PFY{KM7:TR?= MlzwV2FPT0WU
BT-549 cell M{[2Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7iTY5pcWKrdHnvckBw\iCqdX3hckBDXC13NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlc5QDdizszN NVzqcpFSW0GQR1XS
NB17 cell NU\VdZl4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1jVWmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUSuO|g6PzZizszN MX;TRW5ITVJ?
5637 cell M1O5Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvqTY5pcWKrdHnvckBw\iCqdX3hckA2PjN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND63PVY2OiEQvF2= NX7Lb2lxW0GQR1XS
OVCAR-8 cell NHLv[IVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEW0coRKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Njl{NEO2JO69VQ>? MV\TRW5ITVJ?
G-402 cell MmrvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{TDO2lvcGmkaYTpc44hd2ZiaIXtZY4hTy12MEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Mlk{ODN3IN88US=> NHHCS2dUSU6JRWK=
BB30-HNC cell M1L3cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;LcHFuUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwMEeyNVgh|ryP MUPTRW5ITVJ?
HCC1806 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGrBOFJKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G4NFYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjB6M{O5JO69VQ>? NYDkZnAzW0GQR1XS
COLO-800 cell NULnPYdoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4HGVGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24NFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjF{NkSg{txO NWfMWJRMW0GQR1XS
FADU cell NF2xOHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV3C[Ys1UW6qaXLpeIlwdiCxZjDoeY1idiCIQVTVJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4{PjV3NzFOwG0> MYjTRW5ITVJ?
NCI-H1651 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlX4TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjN7NEC5JO69VQ>? M4TRdnNCVkeHUh?=
AGS cell M3fPd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\wVVdMUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlQ4PzFzIN88US=> NUK5TIFkW0GQR1XS
CHP-212 cell MmLiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUjMdlBtUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS5|OUSwPUDPxE1? M3zwZnNCVkeHUh?=
YAPC cell MlyxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJHlCWENiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13LkS3O|EyKM7:TR?= M1jtSXNCVkeHUh?=
GOTO cell MoL4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmPETY5pcWKrdHnvckBw\iCqdX3hckBIV1SRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT60PVU4PiEQvF2= NYD2bYpxW0GQR1XS
KYSE-510 cell NETM[5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGt[W0VvNUGwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU42OTFizszN MlLZV2FPT0WU
NCI-H2342 cell M3K3c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfETY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjV|Mke4JO69VQ>? M2jhT3NCVkeHUh?=
BFTC-905 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3rj[mlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjZ{OEO1JO69VQ>? NX7QOI1NW0GQR1XS
EW-16 cell NHOyO21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4\Y[2lvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlczODl|IN88US=> NYH1PG11W0GQR1XS
SK-MEL-30 cell M1Lae2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPzR3NEOg{txO MmnqV2FPT0WU
HLE cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3L1TGlvcGmkaYTpc44hd2ZiaIXtZY4hUEyHIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT63O|Q5QSEQvF2= NGDnNYdUSU6JRWK=
T98G cell M2TsfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml2wTY5pcWKrdHnvckBw\iCqdX3hckBVQTiJIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT63PVY{PSEQvF2= NV3kXoJPW0GQR1XS
HUTU-80 cell NEj6R4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlSzTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45PDJ{ODFOwG0> NHeyVFJUSU6JRWK=
NOS-1 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIfhS|VKdmirYnn0bY9vKG:oIHj1cYFvKE6RUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46PDd4NjFOwG0> NH7BbnlUSU6JRWK=
SW780 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPKfGpKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU46Pjl2OTFOwG0> MUnTRW5ITVJ?
KYSE-180 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3;pfGlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT2xPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njl5NkW0JO69VQ>? NIW2PXJUSU6JRWK=
MDA-MB-361 cell NEPUcJJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFv2dFdKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk0{PjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lkm4OlQ4KM7:TR?= NY\sZWJ{W0GQR1XS
SNU-C2B cell M3vJNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PMUGlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLVOyRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvODFzM{ig{txO MX7TRW5ITVJ?
NCI-H661 cell NXvpTopJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\nPHpwUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFY3OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwME[5OEDPxE1? M{TKNHNCVkeHUh?=
OE33 cell NH63e2VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG9GOzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14LkG0N|g6KM7:TR?= M3ftS3NCVkeHUh?=
TYK-nu cell NI[ycmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEHUbJFKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOjF6NkOg{txO NFe4SHpUSU6JRWK=
COLO-792 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmfDTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOjV{MUmg{txO MVnTRW5ITVJ?
HEL cell MnO4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVfJcohq[mm2aX;uJI9nKGi3bXHuJGhGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwMk[3OkDPxE1? NYDjVJo2W0GQR1XS
D-566MG cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M37RfWlvcGmkaYTpc44hd2ZiaIXtZY4hTC13Nk\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOzN2OUGg{txO NUK5NXhRW0GQR1XS
U031 cell NXXpboRNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF3RWopKdmirYnn0bY9vKG:oIHj1cYFvKFVyM{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlQyQDF4IN88US=> MX\TRW5ITVJ?
COR-L23 cell MlrZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnuxTY5pcWKrdHnvckBw\iCqdX3hckBEV1JvTEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok41OzN2NjFOwG0> MX3TRW5ITVJ?
NCI-H2452 cell MmjoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIiwdXFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlQ2OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwNUKyPFEh|ryP NF3yTmRUSU6JRWK=
BB65-RCC cell NYfJOoFWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULycZZyUW6qaXLpeIlwdiCxZjDoeY1idiCEQk[1MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwNkS1PUDPxE1? NXvofolDW0GQR1XS
CAL-33 cell NUHoOFBDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoLtTY5pcWKrdHnvckBw\iCqdX3hckBESUxvM{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlY2PjZ3IN88US=> MknzV2FPT0WU

... 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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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.

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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID