ISS840
ISS840 is a selective STAT1 inhibitor, with an IC50 of 31 μM against STAT1 and an IC50 of 560 μM against STAT3. ISS840 is applicable for cancer research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 934750-11-5
- 分子式: C30H33N4O8P
- 分子量:608.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
STAT1 31 μM (IC50) |
STAT3 560 μM (IC50) |
体外実験
ISS840 (30 min) potently inhibits STAT1 homodimerization in nuclear extracts (IC50 = 31 μM), and is 20-fold more selective for STAT1 homodimerization than for STAT3 homodimerization (IC50 = 560 μM)[1].
ISS840 potently and selectively inhibits the DNA-binding activity of STAT1 (IC50 = 31 μM), and shows 20-fold higher specificity for STAT1 over STAT3 in cell-free biochemical assays[2].
ISS840 potently inhibits STAT1 dimerization with an IC50 of 31 μM, which is 20-fold more potent than its inhibitory activity against STAT3 dimerization (IC50 = 560 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 934750-11-5
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分子量 608.58
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分子式 C30H33N4O8P
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SMILES
O=P(O)(O)OC(C=C1)=CC=C1C[C@@H](C(N[C@@H](CC(C)C)C(NC2=CC(OC)=CC=C2)=O)=O)NC(C3=CC=C(C=C3)C#N)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
[1]. Gunning PT, et al. Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains. Bioorganic & medicinal chemistry letters. 2007 Apr 01;17(7):1875-8. [Content Brief]
[2]. Standing D, et al. The Role of STATs in Ovarian Cancer: Exploring Their Potential for Therapy. Cancers. 2023 Apr 26;15(9):2485. [Content Brief]
[3]. Masciocchi D. Design, synthesis and biological evaluation of potential STAT3 inhibitors as anticancer agents. [Content Brief]
[4]. Haque MR. Novel STAT3 small-molecule inhibitors as potential anticancer agents. University of London, University College London (United Kingdom); 2011. [Content Brief]
[5]. Chou PH, et al. A chemical probe inhibitor targeting STAT1 restricts cancer stem cell traits and angiogenesis in colorectal cancer. Journal of biomedical science. 2022 Mar 22;29(1):20. [Content Brief]
[6]. Fletcher S, et al. Molecular approaches towards the inhibition of the signal transducer and activator of transcription 3 (Stat3) protein. ChemMedChem. 2008 Aug;3(8):1159. [Content Brief]
[7]. Berg T, et al. Signal transducers and activators of transcription as targets for small organic molecules. Chembiochem : a European journal of chemical biology. 2008 Sep 01;9(13):2039-44. [Content Brief]
[8]. Shi ZB, et al. Discovery, synthesis, and evaluation of small-molecule signal transducer and activator of transcription 3 inhibitors. Chemical and Pharmaceutical Bulletin. 2012 Dec 1;60(12):1574-80. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)