Molecular Formula | C11H13N5O4 |
Molar Mass | 279.25 |
Density | 1.64 |
Boling Point | 487.6±55.0 °C(Predicted) |
pKa | 6.23±0.42(Predicted) |
Storage Condition | -20℃ |
In vitro study | NSC-207895 decreases both the MDMX mRNA and protein in MCF-7 cells. NSC-207895 induces expression of p53 as well as well-characterized p53-target gene, p21 and MDM2 in a dose-dependent manner in MCF-7 cells. NSC-207895 extends the half-life of p53 from 20 to 30 minutes to more than 3 hours as revealed by cycloheximide chase assays in MCF-7 cells. NSC-207895 also activates p53 and induces p21 and MDM2 expression in LNCaP prostate and A549 lung cancer cells. NSC-207895 increases the mRNA levels of proapoptotic genes including PUMA, BAX, and PIG3 in a dose-dependent manner in MCF-7 cells. NSC-207895 results in a significant increase in the numbers of sub-G0/G1 cells as well as G2 arrest. NSC-207895 also results in more than 40% of cells dying via apoptosis and decreases cell viability in A549 and LNCaP cells. NSC-207895 inhibits biosynthesis of nucleic acids and proteins in L1210 cells. NSC-207895 interactions with DNA repair to activate the DNA defect repair pathway in three species (S. Cereviae, S. pombe and H. sapiens). NSC-207895 acts as cytoxic agent in the G/R-luc astrocytoma cell line with GI50 of 117 nM. NSC-207895 reduced MDMX mRNA and protein in MCF-7 of cells. NSC-207895 dose-dependently induced the expression of p53 in MCF-7 cells, as well as well-characterized p53-target genes, p21 and MDM2. Cycloheximide tracing in MCF-7 cells showed that NSC-207895 extended the Half-Life of p53 from 20-30 minutes to more than 3 hours. In LNCaP prostate cancer and A549 lung cancer cells, NSC-207895 also activated p53 and induced p21 and MDM2 expression. In MCF-7 cells, NSC-207895 dose-dependently increased mRNA levels of pro-apoptotic genes, including PUMA,BAX, and pig3. In A549 and LNCaP cells, NSC-207895 also resulted in more than 40% cell death and decreased cell viability. NSC-207895 inhibition of nucleic acid and protein synthesis in L1210 cells. In three species (S. Cereal, S. pombe and H. sapiens), NSC-207895 interacts with DNA repair to activate DNA damage repair pathways. NSC-207895 is a cytotoxic agent in G/R-luc astrocytoma cell lines, GI50 117 nM. |
biological activity | NSC 207895 inhibits MDMX,IC50 is 2.5 μM, promotes p53 stabilization/activation and DNA damage, and also regulates MDM2(E3 ligase). NSC 207895 (XI-006) inhibits MDMX with IC50 of 2.5 μM, promotes p53 stabilization/activation and DNA damage, and also regulates MDM2(E3 ligase). |
in vitro study | NSC-207895 decreases both the MDMX mRNA and protein in MCF-7 cells. NSC-207895 induces expression of p53 as well as well-characterized p53-target gene, p21 and MDM2, in a dose-dependent manner in MCF-7 cells. NSC-207895 extends the half-life of p53 from 20 to 30 minutes to more than 3 hours as revealed by cycloheximide chase assays in MCF-7 cells. NSC-207895 also activates p53 and induces p21 and MDM2 expression in LNCaP prostate and A549 lung cancer cells. NSC-207895 increases the mRNA levels of proapoptotic genes including PUMA, BAX, and PIG3 in a dose-dependent manner in MCF-7 cells. NSC-207895 results in a significant increase in the numbers of sub-G0/G1 cells as well as G2 arrest. NSC-207895 also results in more than 40% of cells dying via apoptosis and decreases cell viability in A549 and LNCaP cells. NSC-207895 inhibits biosynthesis of nucleic acids and proteins in L1210 cells. NSC-207895 interacts with DNA repair to activate the DNA damage repair pathway in three species (S. cerevisiae, S. pombe and H. sapiens). NSC-207895 acts as cytotoxic agent in the G/R-luc astrocytoma cell line with GI50 of 117 nM. NSC-207895 reduces MDMX mRNA and protein in MCF-7 cells. NSC-207895 dose-dependent induction of p53 in MCF-7 cells, as well as the expression of well-characterized p53-target genes, p21 and MDM2. Cycloheximide tracking assay in MCF-7 cells showed that the half-life of p53 was NSC-207895 prolonged from 20-30 min to more than 3 h. In LNCaP prostate cancer and A549 lung cancer cells, NSC-207895 also activated p53 and induced p21 and MDM2 expression. In MCF-7 cells, mRNA levels of pro-apoptotic genes, including PUMA,BAX, and PIG3, are NSC-207895 in a dose-dependent manner. In A549 and LNCaP cells, NSC-207895 also causes more than 40% cell death and reduces cell activity. NSC-207895 inhibits the synthesis of nucleic acids and proteins in L1210 cells. In three species (S. cerevisiae,S. pombe, and H. sapiens), NSC-207895 interacted with DNA repair to activate the DNA damage repair pathway. NSC-207895 is a cytotoxic agent in G/R-luc astrocytoma cell line with GI50 of 117 nM. |
target | TargetValue p53 MDMX 2.5 μM |
Target | Value |
p53 | |
MDMX | 2.5 μM |