NSC 207895

製品コードS2678 バッチS267802

化学情報

	Synonyms	XI-006	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₁H₁₃N₅O₄
	分子量	279.25	CAS No.	58131-57-0
Solubility (25°C)*	体外	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]

製品説明

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.

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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MCF-7 cell
	濃度	1-10 μM
	反応時間	2 days
	実験の流れ	MCF-7 cells treated with dimethyl sulfoxide (DMSO), nutlin-3a, or NSC-207895 are permeabilized with cold 70% ethanol overnight, and stained with a solution containing 50 μg/mL propidium iodide and 20 μg/mL RNase A at 37°C for 20 minutes. The cells are then subjected to flow cytometry analysis. The FlowJo software is used to calculate percentages of cells in each cell cycle phase. For terminal deoxynucleotidyl transferase–mediated dUTP nick end labeling (TUNEL) staining, 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 according to the manufacturer's protocol. For quantitation, at least 300 cells are randomly chosen and the numbers of TUNEL-positive cells are counted.

参考

[4] Hawes JJ, et al. J Biomol Screen, 2008, 13(8), 795-803.

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カスタマーフィードバック

: Data from [Data independently produced by , , Stem Cell Reports, 2016, 7:1140-1151.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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