Nutlin-3a

For research use only.

Catalog No.S8059 Synonyms: (-)-Nutlin-3

51 publications

Nutlin-3a Chemical Structure

CAS No. 675576-98-4

Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.

Selleck's Nutlin-3a has been cited by 51 publications

Purity & Quality Control

Choose Selective Mdm2 Inhibitors

Biological Activity

Description Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
Features Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.
Targets
p53/MDM2 interaction [3]
(Cell-free assay)
90 nM
In vitro

Nutlin-3a displaces p53 from the binding pocket of MDM2 and thereby releases p53 from inhibition and proteasomal degradation, leading to induction of its downstream targets, cell cycle arrest, and apoptosis. Seven days of incubation with 10 μM nutlin-3a led to >90% inhibition of NIH3T3 cells’ growth[1]. Nutlin-3a stabilizes and activates p53, and induces p21 expression in a dose-dependent manner[1]. Nutlin-3a effectively depletes the S-phase compartment to 0.2-2% and increases the G1- and G2/M-phase compartments[1]. Nutlin-3a induces apoptosis in ~60% of SJSA-1 and MHM cells after 40 h, which increased further after 60 h (85% and 65%, respectively) [1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV-4-11 NFLMW2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrJe3V[UUN3ME2wMlYyOjN5IN88US=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
H4 MoLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\lOW9xUUN3ME2wMlY3OjhizszN NI\rZZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
PA-1 MmS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe3cnk3UUN3ME2wMlg4ODl4IN88US=> MlTWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
NKM-1 NEHkOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPnOFlKSzVyPUGuNFQ6OzFizszN NFXtWG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
NEC8 M33UOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnK[JdKSzVyPUGuNlE2PzJizszN M2m1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
EoL-1-cell NUXTVWoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7FU24yUUN3ME2xMlI3PzBzIN88US=> M17icVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
K5 Mlu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnK0TWM2OD1zLkSyNFczKM7:TR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
QIMR-WIL MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnMXXBKSzVyPUGuOlA5PTRizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
MOLT-16 NHv0SINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGqxRYNKSzVyPUGuO|g3ODRizszN Mn3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
CHP-212 MlTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDNXJNKSzVyPUGuPFE{PjlizszN NFzNNYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
CTB-1 NEfxdnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTNbJBKSzVyPUKuNFIzPDZizszN NFW2Olc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
MOLT-4 M4PNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHH3dHBKSzVyPUKuN|I5PTNizszN MmrmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
A101D Mo\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3h[FNRUUN3ME2yMlM2ODFizszN NULyWoQ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
DOHH-2 NX;EZWlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPaV|dJUUN3ME2yMlQzOjd7IN88US=> Mn:5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
ES4 NYrSXINtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnSTWM2OD1{LkSzNVU2KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
SW780 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr4TlVKSzVyPUKuOVA5QDNizszN MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
VA-ES-BJ MoO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i2O2lEPTB;Mj61OFEyKM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
RPMI-8866 MlvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFK1WGhKSzVyPUKuOVYzOTRizszN MkG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
ML-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1WzPWlEPTB;Mj61OlU4PiEQvF2= NVr3fIpWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
MSTO-211H NXexWoNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\EfGFKSzVyPUKuOVc1PTFizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
JVM-3 Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rI[mlEPTB;Mj61PVMzPCEQvF2= NHi0TIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
A3-KAW Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJwNkG4NVgh|ryP M3qyUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
DK-MG MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H1bGlEPTB;Mj62NlQ4OSEQvF2= NED5T3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
LNCaP-Clone-FGC M2HKdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHKTWM2OD1{Lk[0N|E5KM7:TR?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
HT-144 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37iOGlEPTB;Mj62OFU4PyEQvF2= M2G5NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
NB69 NFTHe3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHtTYhYUUN3ME2yMlY2OzN2IN88US=> M{f4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
A172 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPUZpR{UUN3ME2yMlY4PTh6IN88US=> M3vFUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
RS4-11 NFG1WItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXTTWM2OD1{LkeyOFA4KM7:TR?= NYL4Z3RwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
DU-4475 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTJwN{m1NFIh|ryP MmjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
SJSA-1 NH;2dINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJwOEK1OVYh|ryP MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
BV-173 Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nwNmlEPTB;Mj64OFQ{QSEQvF2= NFnVc5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
U-2-OS MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPET5BqUUN3ME2yMlkyODdizszN NX\0enpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
CHP-134 M{Tyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDKTWM2OD1{LkmzPFgzKM7:TR?= NVrIVnM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
D-502MG NX24c|JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17aWGlEPTB;Mj65O|E2PCEQvF2= NFr0W2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
KS-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jYWmlEPTB;Mz6wNVYzOyEQvF2= Mn7ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
A204 NI\UO|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLhTWM2OD1|LkC1OVg5KM7:TR?= MnP1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+V2FPT0WUPD;hQi=>
KGN NYXMdoJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTNwMEi0PVYh|ryP MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
NCI-H292 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXSTWM2OD1|LkGyNFI5KM7:TR?= M1TKbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
CAKI-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrvNIlKSzVyPUOuNVI3QTRizszN NGPsW|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
C2BBe1 MkPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;SOmlEPTB;Mz6xO|AzPiEQvF2= NILMbZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5USU6JRWK8M4E,
NB10 NXPL[nhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HibmlEPTB;Mz6yNFk3PiEQvF2= M2Di[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
MHH-NB-11 MnXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWzc3hKSzVyPUOuNlY5OjdizszN MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
NCI-SNU-1 NIXOXGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\sTWM2OD1|LkK3PFQ{KM7:TR?= M{\iflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6OTN|ND:nQnNCVkeHUkyvZV4>
HCT-116 NV\i[ZNDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoSzTWM2OD1|LkOwN|M2KM7:TR?= NXLlXlRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
G-401 NHHJRlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDRc|VoUUN3ME2zMlM3OzJ{IN88US=> NUnicXRDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTlzM{O0M{c,W0GQR1XSQE9iRg>?
MN-60 NWKzbG12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlyyTWM2OD1|LkS0NFkzKM7:TR?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7TRW5ITVJ:L3G+
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MCF7 M4G0dGFxd3C2b4Ppd{Bie3OjeR?= M{DSVVMhfU1? NEHyb3MzPCC2bzC3NkBpenN? MmPDTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKEKlbD34V{BmgHC{ZYPzbY9vKGyndnXsJIF1KDNidV2gZYZ1\XJiMkSgeI8hPzJiaILzJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhyMkexOkc,OjN6MEK3NVY9N2F-
MCF7 M13iSWFxd3C2b4Ppd{Bie3OjeR?= MlPoOVAhdk1? MX2yOEB1dyB5MjDodpM> NYLPOWVjUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDv[kBk[XOyYYPlMVMh[2ynYY\h[4UheHKxZIXjeEBifCB3MDDuUUBi\nSncjCyOEB1dyB5MjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqew>? NFrkTmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iwNlcyPid-MkO4NFI4OTZ:L3G+
MCF7 MUfD[YxtKGO7Y3zlJIF{e2G7 NWjuNnVpOyC3TR?= NGjOfWEzPCC2bzC3NkBpenN? MYPD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDheEBIOC:JMTDwbIF{\SCjdDCzJJVOKGGodHXyJFI1KHSxIEeyJIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKE[DQ2OgZY5idHm|aYO= M{K1N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OECyO|E3Lz5{M{iwNlcyPjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / MDM2 / p21 / Bax / Bak / Noxa / cleaved caspase / pro-caspase; 

PubMed: 16014563     


Expression of apoptosis- and cell-cycle–associated proteins in OCI-AML-3 cells, which were treated with 5 μM Nutlin-3a for the indicated times. Nutlin-3a induced increased protein expression of p53, MDM2, and p21 in OCI-AML-3 cells in a time-dependent fashion. Nutlin-3a induced Noxa, a BH3-only member of the Bcl-2 family, followed by caspase activation. β-actin was used to confirm equal loading of proteins. Arrowheads indicate cleared caspases.

BMI-1; 

PubMed: 26887044     


Western blot analysis of BMI-1 and actin was performed in BV-173, SUP-B15, NALM-6, NALM-19 and REH cell lines after 24 hours treatment with increasing concentrations of Nutlin-3a (1 μM, 2 μM, 5 μM) and with DMSO control. 

p53-Ser15 / p53-Ser37 / p53-Lys382 / MDM2 / CDC2 / PLK1 / HSC70; 

PubMed: 23666059     


Expression of the indicated proteins in whole-cell lysates of cells treated for 96 h with 50 μM resveratrol (R), 5 μM nutlin-3a (N), or co-treated with both substances (RN).

16014563 26887044 23666059
Immunofluorescence
p-p21 / β-actin; 

PubMed: 31083332     


Cells were treated with fluoride (5 mM) with/without Nutlin-3a for 24 h. p-p21 (green), nucleus (DAPI; blue) and β-actin (red) expression were detected by immunocytochemistry. Nutlin-3a addition augmented p-p21 expression compared to NaF treatment alone.

P53; 

PubMed: 21394100     


At 12 h following treatment with nutlin-3a, DoHH2 and MCA cells had increased levels of p53 visualized by immunofluorescence. p53 localization was predominantly nuclear. The 4',6-diamidino-2-phenylindole was used as counterstain of the nuclei.

Ac-p300; 

PubMed: 30240745     


HepG2 cells were treated with 5 μM Nutlin-3a for 24 hr, and the levels of Ac-p300 and p53 were assessed by co-immunofluorescence. Fluorescence intensity of Ac-p300 in control cells versus Nutlin-3a-treated cells have been quantified (represented as mean ± SD, unpaired two-tailed Student's t test, n = 50 of three independent experiments). Scale bar, 10 μm.

31083332 21394100 30240745
Growth inhibition assay
Cell viability; 

PubMed: 26248031     


All 15 cell lines were plated in 96-well plates. After 24h, media was exchanged and cells were treated with incremental concentrations of Nutlin-3a (1 μM, 5 μM, 10 μM, 25 μM, 50 μM, and 70 μM). After 72h of Nutlin-3a treatment, cell viability was measured by WST assay and compared to untreated control.

26248031
In vivo Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage [1]. Nutlin-3 is a selective activator of the p53 pathway in vivo and highly efficacious against SJSA-1 osteosarcoma tumors[1]. Tumors with wild-type p53 and mdm2 gene amplification will respond best to therapy with Nutlin-3a.

Protocol

Kinase Assay:[3]
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Biacore studies:

Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel
Cell Research:[2]
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  • Cell lines: OSA, T778, RMS13, U2OS, SaOS-2
  • Concentrations: ~5 μM
  • Incubation Time: 120 h
  • Method: SRB
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: SJSA-1 xenograft
  • Dosages: 50, 100, 200 mg/kg twice daily
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (171.97 mM)
Water Insoluble
Ethanol '100 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.
10mg/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 581.49
Formula

C30H30Cl2N4O4

CAS No. 675576-98-4
Storage powder
in solvent
Synonyms (-)-Nutlin-3
Smiles CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    What is the difference between S1061 (Nutlin-3) and S8059 (Nutlin-3a)?

  • Answer:

    S1061 is a racemic mixture of Nutlin3a and Nutlin3b. s8059 is the active enantiomer of Nutlin3.

Mdm2 Signaling Pathway Map

Related Mdm2 Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID