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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
STAT1 31 μM (IC50) |
STAT3 560 μM (IC50) |
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.
化学情報
-
CAS 番号 934750-11-5
-
分子量 608.58
-
分子式 C30H33N4O8P
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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)