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NSC-207895 (XI-006) is a derivative of nitrobenzofuroxan and an anticancer agent with an EC50 of 1 μM. NSC-207895 (XI-006) is a highly electrophilic compound known to have both antitumor and mutagenic activities. NSC-207895 (XI-006) may lead to the damage of DNA that inhibits the growth of tumors. NSC-207895 (XI-006) strikingly prevented the expression of MDMX which is a p53-binding protein and modulate the activities and stabilities of p53. NSC-207895 (XI-006) is less toxic and reduced the activities of MDMX promoter in a dose-dependent manner. Moreover,NSC-207895 (XI-006) possibly decreased the expression of MDMX via suppressing MDMX transcription. However, NSC-207895 (XI-006) induced the expression of MDM2 which is also a p53 downstream gene, despite to a less extent. In addition, NSC-207895 (XI-006) also upregulated the expression of p53 in MCF-7 cells that led to increased expression of proapoptotic genes including PUMA, BAX, as well as PIG3. Notably, NSC-207895 (XI-006), also called a small-molecule p53 activator, gives rise to MCF-7 cells to experience apoptosis and decrease the viability of cancer cells along with nutlin-3a, which dissociated the MDM2-p53 complex.
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cell |
| Preparation method | Treating MCF-7 cells with dimethyl sulfoxide (DMSO), nutlin-3a, or NSC-207895 are permeabilized with cold 70% ethanol overnight, and staining with a solution containing 50 μg/mL propidium iodide and 20 μg/mL RNase A at 37°C for 20 minutes. And then subjected the cells to flow cytometry analysis. Using the FlowJo software to calculate percentages of cells in each cell cycle phase. For terminal deoxynucleotidyl transferase–mediated dUTP nick end labeling (TUNEL) staining,according to the manufacturer's protocol, MCF-7 cells treated with the NSC-207895 for 2 days are fixed with 4% paraformadelhyde for 1 hour, and then subjected to dUTP labeling using In Situ Cell Death Detection Kit TMR Red . For quantitation, choose at least 300 cells randomly and count the numbers of TUNEL-positive cells . |
| Concentrations | 1-10 μM |
| Incubation time | 2 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 279.25 |
| Formula | C11H13N5O4 |
| CAS Number | 58131-57-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mdm2 Products |
|---|
| Nutlin-3
Nutlin-3 is a selective MDM2 (mouse double minute 2) antagonist with IC50 of 90 nM. Nutlin-3 induces apoptosis in cancer cells. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM in cells with wild-type p53 such as HCT116, RKO and SJSA-1. |
| NSC 66811
NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. |
| Nutlin-3a
Nutlin-3a, the active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits the p53/MDM2 interaction with IC50 of 90 nM. |
| Nutlin-3b
Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite enantiomer Nutlin-3a. |
| SL-01
SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM. |
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