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Formula | C11H13N5O4 |
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Molecular Weight | 279.25 | CAS No. | 58131-57-0 | |
Solubility (25°C)* | In vitro | 5%TFA | 6 mg/mL (21.48 mM) | |
DMSO | 0.4 mg/mL (1.43 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. | ||
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In vitro | 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. [1] NSC-207895 inhibits biosynthesis of nucleic acids and proteins in L1210 cells. [2] NSC-207895 interacts with DNA repair to activate the DNA damage repair pathway in three species (S. cerevisiae, S. pombe and H. sapiens). [3] NSC-207895 acts as cytotoxic agent in the G/R-luc astrocytoma cell line with GI50 of 117 nM. [4] |
Cell Assay: |
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Data from [Data independently produced by , , Stem Cell Reports, 2016, 7:1140-1151.]
Integrated drug response prediction models pinpoint repurposed drugs with effectiveness against rhabdomyosarcoma [ PLoS One, 2024, 19(1):e0295629] | PubMed: 38277404 |
125I Seed Promotes Apoptosis in Non-small Lung Cancer Cells via the p38 MAPK-MDM2-p53 Signaling Pathway [ Front Oncol, 2021, 11:582511] | PubMed: 33968713 |
MDM2 and MDMX promote ferroptosis by PPARα-mediated lipid remodeling. [ Genes Dev, 2020, 34(7-8):526-543] | PubMed: 32079652 |
Identification of Mubritinib (TAK 165) as an inhibitor of KSHV driven primary effusion lymphoma via disruption of mitochondrial OXPHOS metabolism [ Oncotarget, 2020, 11(46):4224-4242] | PubMed: 33245718 |
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897] | PubMed: 30760778 |
MiR-370 promotes apoptosis in colon cancer by directly targeting MDM4. [ Oncol Lett, 2018, 15(2):1673-1679] | PubMed: 29434862 |
The protective effect of PFTα on alcohol-induced osteonecrosis of the femoral head [ Oncotarget, 2017, 8(59):100691-100707] | PubMed: 29246013 |
The protective effect of PFTα on alcohol-induced osteonecrosis of the femoral head [ Oncotarget, 2017, 8(59):100691-100707] | PubMed: 29246013 |
Inhibiting the SUMO Pathway Represses the Cancer Stem Cell Population in Breast and Colorectal Carcinomas. [ Stem Cell Reports, 2016, 7(6):1140-1151] | PubMed: 27916539 |
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