JN122
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis.
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- CAS 番号: 3035577-19-3
- 分子式: C33H37Cl2N3O4
- 分子量:610.57
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
IC50: 39.6 nM (HCT-116 cells); 4.28μM (HEK-293 cells)[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.9 nM
Compound: (-)60; JN122
|
Growth inhibition of human A549 cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human A549 cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| HCT-116 | IC50 |
<1 nM
Compound: (-)60; JN122
|
Antiproliferative activity against human HCT-116 cells harboring p53 assessed inhibition of cell growth incubated for 4 days by celltiter-glo assay
Antiproliferative activity against human HCT-116 cells harboring p53 assessed inhibition of cell growth incubated for 4 days by celltiter-glo assay
|
[PMID: 38062557] |
| HCT-116 | IC50 |
13.6 nM
Compound: XVI; JN122
|
Antiproliferative activity against human HCT-116 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human HCT-116 cells incubated for 4 days by CCK8 assay
|
[PMID: 38581730] |
| HeLa | IC50 |
12.24 nM
Compound: (-)60; JN122
|
Growth inhibition of human HeLa cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human HeLa cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| HepG2 | IC50 |
0.32 nM
Compound: (-)60; JN122
|
Growth inhibition of human HepG2 cells harboring p53 incubated for 4 days by celltiter glo assay
Growth inhibition of human HepG2 cells harboring p53 incubated for 4 days by celltiter glo assay
|
[PMID: 38062557] |
| MOLM-13 | IC50 |
49.9 nM
Compound: (-)60; JN122
|
Growth inhibition of human MOLM-13 cells incubated for 2 days by CCK-8 assay
Growth inhibition of human MOLM-13 cells incubated for 2 days by CCK-8 assay
|
[PMID: 38062557] |
| MOLM-13 | IC50 |
0.2 nM
Compound: XVI; JN122
|
Antiproliferative activity against human MOLM-13 cells incubated for 2 days by CCK8 assay
Antiproliferative activity against human MOLM-13 cells incubated for 2 days by CCK8 assay
|
[PMID: 38581730] |
| MSTO-211H | IC50 |
9.48 nM
Compound: (-)60; JN122
|
Growth inhibition of human MSTO-211H cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human MSTO-211H cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| NCI-H460 | IC50 |
0.26 nM
Compound: (-)60; JN122
|
Growth inhibition of human NCI-H460 cells harboring p53 incubated for 4 days by CCK-8 assay
Growth inhibition of human NCI-H460 cells harboring p53 incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
| SW480 | IC50 |
7.1 nM
Compound: (-)60; JN122
|
Growth inhibition of human SW480 cells incubated for 4 days by CCK-8 assay
Growth inhibition of human SW480 cells incubated for 4 days by CCK-8 assay
|
[PMID: 38062557] |
化学情報
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CAS 番号 3035577-19-3
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分子量 610.57
-
分子式 C33H37Cl2N3O4
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SMILES
CCN1[C@H]([C@@H]([C@@]2([C@@H]1CC(C)(C)C)CNC3=CC(Cl)=CC=C32)C4=CC(Cl)=CC=C4)C(NC5=CC=C(C=C5OC)C(O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)