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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- CAS No.: 934750-11-5
- Formule: C30H33N4O8P
- Masse moléculaire:608.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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.
Chemical Information
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CAS No. 934750-11-5
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Masse moléculaire 608.58
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ISS840 Related Classifications
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