|4-[[4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮|CsnPharm

CAS No.: 890090-75-2

4-(4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one Catalog No. CSN12388

Synonyms: Nutlin 3(Random Configuration)

Nutlin 3(Random Configuration) is an MDM2 antagonist which can activate p53 pathway through inhibition of p53-MDM2 interaction.

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实验方案

技术信息

生物活性

靶点 MDM2

IC50:90nM
描述MDM2 binds the p53 tumor suppressor protein with high affinity and negatively modulates its transcriptional activity and stability. Overexpression of MDM2, found in many human tumors, effectively impairs p53 function. Inhibition of MDM2-p53 interaction can stabilize p53 and may offer a novel strategy for cancer therapy^[3]. Nutlin 3a is the active enantiomer of nutlin-3, inhibiting the p53/MDM2 interaction, and IC50 was 90 nM in the cell-free test^[4]. In vitro, Nutlin-3a replaces p53 from the binding pocket of the MDM2 protein, thereby releasing p53 from a state of inhibition and proteasome degradation, leading to induction of downstream targets, cell cycle arrest and apoptosis. Incubation for 10 μM Nutlin-3a for 7 days resulted in growth inhibition of NIH3T3 cells of over 90%^[5]. Nutlin-3a effectively reduced S-phase cells to 0.2-2% and increased G1- and G2/M- phase cells^[5]. After 40 h, Nutlin-3a induced apoptosis in about 60% of SJSA-1 and MHM cells, while at 60 h, the apoptotic cells reached 85% and 65%, respectively^[5]. In vivo, Nutlin-3a inhibits xenograft growth in a dose-dependent manner, showing large tumor contractions at the highest dose (200 mg/kg). Nutlin-3a is a selective activator of the p53 pathway in vivo and highly effective against SJSA-1 osteosarcoma. Tumors with wild-type p53 and MDM2 amplification responded best to nutlin-3a therapy^[5].
作用机制Nutlin 3 binds MDM2 in the p53-binding pocket ^[2].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
115	0.5-10 μM	Cell Viability Assay	0-6 d	inhibits proliferation in a dose-dependent manner	25067787
115	0.5/1/5 μM	Function Assay	48 h	leads to increased expression of p53 and some p53 target genes: MDM2, and p21	25067787
115	5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	25067787

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7197 mL
- 8.5986 mL
- 17.1972 mL
- 5 mM
- 0.3439 mL
- 1.7197 mL
- 3.4394 mL
- 10 mM
- 0.1720 mL
- 0.8599 mL
- 1.7197 mL

技术信息

CAS号

890090-75-2

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H30Cl2N4O4

运输

蓝冰

分子量

581.49

别名

Nutlin 3(Random Configuration)

溶解度

DMSO	100.0 mg/mL (172.0 mM)
Water	Insoluble
Ethanol	30.0 mg/mL (51.6 mM)

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

115	0.5-10 μM	Cell Viability Assay	0-6 d	inhibits proliferation in a dose-dependent manner	25067787
115	0.5/1/5 μM	Function Assay	48 h	leads to increased expression of p53 and some p53 target genes: MDM2, and p21	25067787
115	5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	25067787
115	5 μM	Function Assay	48 h	induces p53-dependent senescence	25067787
117	0.5-10 μM	Cell Viability Assay	0-6 d	inhibits proliferation in a dose-dependent manner	25067787
A2780	10 μM	Function Assay	21h	increases p53 protein levels	25426548
A2780	10 μM	Function Assay	21h	decreases the FoxM1 levels	25426548
A2780	5/10/20 μM	Function Assay	24 h	upregulates p53, MDM2, p21 and DR5 protein levels dose dependently	24136147
A2780	5/10/20 μM	Apoptosis Assay	24 h	enhances apoptosis induction by D269H/E195R over rhTRAIL	24136147
A498	0.5-10 μM	Cell Viability Assay	0-6 d	inhibits proliferation in a dose-dependent manner	25067787
A498	0.5/1/5 μM	Function Assay	48 h	leads to increased expression of p53 and some p53 target genes: MDM2, and p21	25067787
A498	5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	25067787
A498	5 μM	Function Assay	48 h	induces p53-dependent senescence	25067787
A549	-	Growth Inhibition Assay	24 h	IC50=17.68 ± 4.52 μM	26125230
A549-920	-	Growth Inhibition Assay	24 h	IC50=33.85 ± 4.84 μM	26125230
A549-NTC	-	Growth Inhibition Assay	24 h	IC50=19.42 ± 1.96 μM	26125230
ACHN	0.5-10 μM	Cell Viability Assay	0-6 d	inhibits proliferation in a dose-dependent manner	25067787
ACHN	0.5/1/5 μM	Function Assay	48 h	leads to increased expression of p53 and some p53 target genes: MDM2, and p21	25067787
ACHN	5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	25067787
ACHN	5 μM	Function Assay	48 h	induces p53-dependent senescence	25067787
AML2	2/10 μM	Apoptosis Assay	24/48 h	induces apoptosis	24659749
AML2	10μM	Function Assay	2/4 h	increases the level of p53	24659749
AML3	10μM	Function Assay	2/4 h	increases the level of p53	24659749
AT2	5/10 μM	Function Assay	-	leads to a substantial accumulation of the p53 protein as well as the expression of its direct targets p21, MDM2 and the pro-apoptotic BAX and PUMA proteins	24240203
AT2	0-25 μM	Cell Viability Assay	-	inhibits cell viability dose dependently	24240203
BeWo	30 µM	Function Assay	24 h	increases p53, Mdm2, p21 and Puma at the protein level	24498154
BeWo	30 µM	Apoptosis Assay	24 h	increases apoptosis	24498154
C2C12	10 μM	Growth Inhibition Assay	24/48/72 h	inhibits cells proliferation and differentiation	25871794
C666-1	-	Growth Inhibition Assay	-	IC50=19.95±8.93 μM	26252575
C666-1	10 µM	Cell Viability Assay	48 h	sensitizes C666-1 cells to the cytotoxic effect of cisplatin	26252575
C666-1	10 µM	Function Assay	24 h	activates the p53 pathway, upregulating p53, p21 and Mdm2	26252575
C666-1	10 µM	Apoptosis Assay	48/72 h	sensitizes C666-1 cells to cisplatin-induced apoptosis	26252575
Caki-2	0.5-10 μM	Cell Viability Assay	0-6 d	inhibits proliferation in a dose-dependent manner	25067787
Caki-2	0.5/1/5 μM	Function Assay	48 h	leads to increased expression of p53 and some p53 target genes: MDM2, and p21	25067787
Caki-2	5 μM	Growth Inhibition Assay	48 h	induces cell cycle arrest	25067787
Caki-2	5 μM	Function Assay	48 h	induces p53-dependent senescence	25067787
CRL-5908	-	Growth Inhibition Assay	24 h	IC50=38.71 ± 2.43 μM	26125230
DU4475	5/10/20 μM	Function Assay	24 h	downregulates Toca-1 dose dependently	25547174
H460	5/10/20 μM	Function Assay	24 h	upregulates p53, MDM2, p21 and DR5 protein levels dose dependently	24136147
H460	5/10/20 μM	Apoptosis Assay	24 h	enhances apoptosis induction by D269H/E195R over rhTRAIL	24136147
HCT116	10 µM	Function Assay	24 h	causes a p53-dependent tetraploid G1-arrest in diploid HCT116 clones D3 and D8	25380055
Hep3B	-	Growth Inhibition Assay	72 h	IC50=20.18 ± 1.84 μM	24884809
Hep3B	-	Apoptosis Assay	-	induces apoptosis	24884809
HepG2	-	Growth Inhibition Assay	72 h	IC50=35.86 ± 2.9 μM	24884809
HepG2	-	Apoptosis Assay	-	induces apoptosis	24884809
HepG2/As	-	Growth Inhibition Assay	72 h	IC50=68.13 ± 9.6 μM	24884809
Huh-7	-	Growth Inhibition Assay	72 h	IC50=33.96 ± 3.9 μM	24884809
Huh-7	-	Apoptosis Assay	-	induces apoptosis	24884809
HuH-7	1.25-20 μM	Cell Viability Assay	24/48/72 h	inhibits cell proliferation dose and time dependently	24286312
HuH-7	20 μM	Apoptosis Assay	48 h	induces apoptosis	24286312
HuH-7	10 μM	Function Assay	36 h	down-regulates the protein expression level of phospho-Ser392-p53	24286312
L6	10 μM	Growth Inhibition Assay	24/48/72 h	inhibits cells proliferation and differentiation	25871794
Lovo	5/10/20 μM	Function Assay	24 h	upregulates p53, MDM2, p21 and DR5 protein levels dose dependently	24136147
Lovo	5/10/20 μM	Apoptosis Assay	24 h	enhances apoptosis induction by D269H/E195R over rhTRAIL	24136147
MCF-10A1	10 μM	Function Assay	24/48 h	inhibits migration of normal breast epithelial	25257729
MCF-10CA1a	10 μM	Function Assay	48 h	inhibits basal invasion and reduced TGF-β3-induced invasion to basal levels	25257729
MCF-10CA1a	10 μM	Function Assay	24 h	decreases the TGF-β3-induced mRNA levels ofMMP2, MMP9, and integrin β 3	25257729
MCF-10CA1a	10 μM	Function Assay	24 h	inhibits TGF-β3-induced EPHB2 mRNA and protein expression	25257729
MCF7	5 μM	Growth Inhibition Assay	48 h	blocks 27-OHC-induced cell proliferation comparable to that of basal levels	26350565
MCF7	2.5 µM	Cell Viability Assay	5 d	sensitizes MCF7 to PARP inhibition	25085902
MCF7	2.5 µM	Function Assay	48 h	decreases the homologous DSB repair frequencies	25085902
MCF-7	10 μM	Function Assay	-	inhibits cyclin D1 and Dicer	25702703
MCF-7	10 μM	Function Assay	0-24 h	induces p53 and p21/Cip1	25482373
MOLM	10 μM	Function Assay	24 h	upregulates the SOCS-1 expression	24473562
MOLM-13	6 μM	Function Assay	0-8 h	increases the levels of p53, MDM2, p21 and acetylated p53	24885082
MOLM-13	6 μM	Function Assay	6 h	enhances the acetylation of histone H2B and heat shock proteins Hsp27 and Hsp90	24885082
MOML13	2/10 μM	Apoptosis Assay	24/48 h	induces apoptosis	24659749
MOML13	10μM	Function Assay	2/4 h	increases the level of p53	24659749
NCI-H23	10 μM	Function Assay	21h	increases p53 protein levels	25426548
NCI-H23	10 μM	Function Assay	21h	decreases the FoxM1 levels	25426548
NP460	-	Growth Inhibition Assay	-	IC50=22.85±1.18 μM	26252575
NP69	-	Growth Inhibition Assay	-	IC50=31.69±2.54 μM	26252575
OCI	10 μM	Function Assay	24 h	upregulates the SOCS-1 expression	24473562
OVCAR10	10 μM	Function Assay	21h	increases p53 protein levels	25426548
RAW 264.7	10 μM	Function Assay	30 min	prevents the p53 reduction in response to LPS	25172547
RAW 264.7	10 μM	Function Assay	30 min	reduces the LPS-augmented the NF-κB luciferase reporter gene activity	25172547
RAW 264.7	10 μM	Function Assay	30 min	inhibits LPS-induced NO production	25172547
REH	5/10 μM	Function Assay	-	leads to a substantial accumulation of the p53 protein as well as the expression of its direct targets p21, MDM2 and the pro-apoptotic BAX and PUMA proteins	24240203
REH	0-25 μM	Cell Viability Assay	-	inhibits cell viability dose dependently	24240203
RKO	20 μM	Function Assay	24 h	increases the levels of the HO-1 protein as well as the p53 protein	24366007
RKO	20 μM	Function Assay	24 h	induces HO-1 expression at the level of transcription	24366007
SK-BR-7	10 μM	Function Assay	24 h	inhibits TGF-β3-induced EPHB2 mRNA and protein expression	25257729
SMMC7721	-	Growth Inhibition Assay	72 h	IC50=31.28 ± 4.2 μM	24884809
SMMC7721	-	Apoptosis Assay	-	induces apoptosis	24884809
SMMC-7721	10 μM	Function Assay	48 h	causes DNA DSB damage	25544361
SMMC-7721	10 μM	Function Assay	48 h	induces the chromatin-bound protein IFI16 to partially localize in the cytoplasm	25544361
SMMC-7721	10 μM	Function Assay	48 h	increases the expression level of IFNB1 mRNA	25544361
SMMC-7721	10 μM	Function Assay	36 h	causes the ectopic expression of IFI16	25544361
SMMC-7721	1.25-20 μM	Cell Viability Assay	24/48/72 h	inhibits cell proliferation dose and time dependently	24286312
SMMC-7721	20 μM	Apoptosis Assay	48 h	induces apoptosis	24286312
SMMC-7721	10 μM	Function Assay	36 h	down-regulates the protein expression level of phospho-Ser392-p53	24286312
SMMC7721/Ac	-	Growth Inhibition Assay	72 h	IC50=55.21 ± 5.03 μM	24884809
SUM102PT	10 μM	Function Assay	24 h	inhibits TGF-β3-induced EPHB2 mRNA and protein expression	25257729
U2OS	20 μM	Function Assay	24 h	increases the mRNA levels of BCL2A1, BCLXL andBCLW	24867259
U2OS	20 μM	Function Assay	24 h	increases the levels of the HO-1 protein as well as the p53 protein	24366007
U2OS	20 μM	Function Assay	24 h	induces HO-1 expression at the level of transcription	24366007
UoCB6	5/10 μM	Function Assay	-	leads to a substantial accumulation of the p53 protein as well as the expression of its direct targets p21, MDM2 and the pro-apoptotic BAX and PUMA proteins	24240203
UoCB6	0-25 μM	Cell Viability Assay	-	inhibits cell viability dose dependently	24240203

4-(4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one Catalog No. CSN12388

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