NSC697923

製品コードS7142 バッチS714201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₁H₉NO₅S

分子量

267.26

CAS No.

343351-67-7

Solubility (25°C)*

体外

DMSO

53 mg/mL (198.3 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

2.65mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 53 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
in vitro	NSC697923 selectively inhibits PMA-induced NF-κB activation, and also inhibits IκBα phosphorylation by both RANKL and LPS. NSC697923 impedes the formation of the Ubc13 and ubiquitin thioester conjugate and suppresses constitutive NF-κB activity in ABC-DLBCL cells. In addition, NSC697923 inhibits the proliferation and survival of ABC-DLBCL cells and GCB-DLBCL cells, and also induces apoptosis of primary DLBCL cells. ^[1] In neuroblastoma (NB) cell lines, NSC697923 shows cytotoxic effect, and inhibits both anchorage-dependent and -independent colony formation. ^[2]
in vivo	NSC697923 (5 mg/kg/day, i.p.) demonstrates potent antitumor efficacy in both NB SH-SY5Y and NGP xenografts. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro ubiquitination assay
キナーゼアッセイ	The reactions are carried out at 37°C for 40 minutes in a buffer containing 50mM Tris-HCl, pH 7.5, 5mM MgCl₂, 200μM ATP, 120μM Ub (U-100H), and 0.1μM E1 (E-304). For Ubc13-mediated Ub chain synthesis, the reaction mixture includes 0.2 μM Ubc13 (E2-600) and 0.2 mM Uev1A (E2-662) with or without GST-TRAF6. For UbcH5c-catalyzed ubiquitination, UbcH5c (E2-627) instead of Ubc13 and Uev1A is used in the reaction. Compound NSC697923 is added into the reaction mixtures at the indicated concentrations. The reactions are terminated with an equal volume of SDS-PAGE sample buffer and the products are analyzed by Western blotting with a Ub-specific antibody. For detecting the E2-Ub (Ubc13∼Ub or UbcH5c∼Ub) thioester conjugates, the reactions are carried out as described in “In vitro ubiquitination assay” without GST-TRAF6. The reactions are terminated by the addition of the SDS-PAGE sample buffer without a reducing agent unless specified. The products are analyzed by Western blotting with an anti-Ubc13 or anti-UbcH5c antibody.
細胞アッセイ	細胞株	BC-DLBCL, GCB-DLBCL and primary DLBCL cells.
	濃度	~1 μM
	反応時間	24 hours
	実験の流れ	Cell viability is measured by trypan blue exclusion assay following the manufacturer's instructions.
動物実験	動物モデル	SH-SY5Y and NGP xenografts.
	投薬量	~5 mg/kg/day
	投与方法	i.p.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , FASEB J, 2017, 31(1):308-319]

: Data from [Data independently produced by , , J Mol Med (Berl), 2018, 96(7):645-659]

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：

CRISPR-Cas9 knockout screen identifies novel treatment targets in childhood high-grade glioma [ Clin Epigenetics, 2023, 15(1):80]	PubMed: 37161535
Enzymatic Redox Properties and Cytotoxicity of Irreversible Nitroaromatic Thioredoxin Reductase Inhibitors in Mammalian Cells [ Int J Mol Sci, 2023, 24(15)12460]	PubMed: 37569833
Darapladib, an inhibitor of Lp-PLA2, sensitizes cancer cells to ferroptosis by remodeling lipid metabolism [ bioRxiv, 2023, 10.1101/2023.04.08.536136]	PubMed: None
A small molecule inhibitor of caspase-1 inhibits NLRP3 inflammasome activation and pyroptosis to alleviate gouty inflammation [ Immunol Lett, 2022, 244:28-39]	PubMed: 35288207
RNF8-mediated regulation of Akt promotes lung cancer cell survival and resistance to DNA damage [ Cell Rep, 2021, 37(3):109854]	PubMed: 34686341
Ubiquitination status does not affect Vps34 degradation [ Genes Dis, 2020, 7(3):401-407]	PubMed: 32884994
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143]	PubMed: 33067904
Chilling stress reduced protein translation by the ubiquitination of ribosomal proteins in Volvariella volvacea. [ J Proteomics, 2020, 215:103668]	PubMed: 31982547
Ube2v1-mediated ubiquitination and degradation of Sirt1 promotes metastasis of colorectal cancer by epigenetically suppressing autophagy [Shen T J Hematol Oncol, 2018, 11(1):95]	PubMed: 30016968
UBE2N Promotes Melanoma Growth via MEK/FRA1/SOX10 Signaling [ Cancer Res, 2018, 78(22):6462-6472]	PubMed: 30224375

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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