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.
For research use only. We do not sell to patients.
- CAS No.: 934750-11-5
- Formula: C30H33N4O8P
- Molecular Weight:608.58
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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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Molecular Weight 608.58
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
HY-186227 Related Classifications
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