ISRIB (trans-isomer)

製品コードS7400 バッチS740002

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式
C22H24Cl2N2O4
 
 
分子量 451.34 CAS No. 1597403-47-8
Solubility (25°C)* 体外 DMSO 5 mg/mL (11.07 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 95% Corn oil
0.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 2 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 ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells.
in vitro

ISRIB blocks production of endogenous ATF4, whereas XBP1 mRNA splicing and XBP1s production persisted. ISRIB prevents cells from re-establishing ER homeostasis by blocking signaling through the PERK branch of the UPR, and decreases the viability of cells that are subjected to ER-stress. [1]
in vivo

ISRIB shows favorable properties in pharmacokinetic profiling experiments and good bioavailability in vivo. ISRIB (0.25 mg/kg i.p.) increases long-term memory in mice by enhancing spatial and fear-associated learning. [1]

プロトコル(参考用のみ)

キナーゼアッセイ High-content microscopy-based secondary screen [1]
U2OS cells carrying the ATF4-dGFP-IRES-Cherry reporter are plated in 96 well plates and treated with 100 nM Thapsigargin and 10μM of the cherry-picked compounds for 8 hr. Cells are stained with Hoechst 33,258 and are visualized using an automated microscope. Data acquisition and image analyses are performed with the INCell Developer Toolbox Software, version 1.9. Compounds that block induction of the ATF4-dGFP reporter, do not block the accumulation of mCherry downstream of the IRES, and are deemed non-toxic as determined by cell number measured by counting nuclei, are repurchased for further analyses.
細胞アッセイ 細胞株 Cell-free assays
濃度 5 nM
反応時間
実験の流れ
動物実験 動物モデル Male C57BL/6J mice
投薬量 0.25 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Development, 2017, 144(1):128-138]

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：

Neurodegeneration Risk Factor, EIF2AK3 (PERK), Influences Tau Protein Aggregation [ J Biol Chem, 2022, S0021-9258(22)01264-9] PubMed: 36563857
5-Azacitidine Induces NOXA to Prime AML Cells for Venetoclax-mediated Apoptosis. [ Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-1900] PubMed: 32054729
Intracellular XBP1-IL-24 Axis Dismantles Cytotoxic Unfolded Protein Response in the Liver [ Cell Death Dis, 2020, 6;11(1):17] PubMed: 31907348
Sphingolipid Modulation Activates Proteostasis Programs to Govern Human Hematopoietic Stem Cell Self-Renewal. [ Cell Stem Cell, 2019, 25(5):639-653] PubMed: 31631013
Translation repression by maternal RNA binding protein Zar1 is essential for early oogenesis in zebrafish [Miao L, et al. Development, 2017, 144(1):128-138] PubMed: 27913641
Role of Endoplasmic Reticulum Stress in Learning and Memory Impairment and Alzheimer's Disease-Like Neuropathology in the PS19 and APPSwe Mouse Models of Tauopathy and Amyloidosis [ eNeuro, 2017, 4(4)ENEURO.0025-17.2017] PubMed: 28721361
Role of Endoplasmic Reticulum Stress in Learning and Memory Impairment and Alzheimer's Disease-Like Neuropathology in the PS19 and APPSwe Mouse Models of Tauopathy and Amyloidosis. [ eNeuro, 2017, 4(4)] PubMed: 28721361

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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