1456632-40-8 Usage
Description
SH-4-54 is an inhibitor of signal transducer and activator of transcription 3 (STAT3) with an IC50 of 4.7 μM for STAT3 homodimer DNA binding activity. It selectively inhibits STAT3 homodimer over STAT1 and STAT5 homodimer and STAT3:STAT1 heterodimer DNA binding in EGF-stimulated NIH3T3/hEGFR nuclear extracts containing activated STAT1, STAT3, and STAT5. SH-4-54 also decreases STAT3 iNOS, Survivin, and Bcl-2 promoter occupancy in MDA-MB-231 cells.
Uses
Used in Cancer Treatment:
SH-4-54 is used as an inhibitor for STAT3, which is unusually active in glioblastoma and plays a crucial role in tumor growth. It is effective against glioma, breast, and prostate cancer cell lines that express constitutively active STAT3, with IC50s ranging from 1-7.4, 3.8-4.5, and 5.3-5.8 μM, respectively.
Used in Drug Delivery Systems:
In vivo, SH-4-54 (3 mg/kg per day) has been shown to inhibit tumor growth in the U251MG glioma and MDA-MB-231 breast cancer mouse xenograft models. This suggests its potential use in drug delivery systems for targeted cancer therapy.
Used in Pharmaceutical Research:
SH-4-54's ability to selectively inhibit STAT3 homodimer and its effects on various cancer cell lines make it a valuable compound for pharmaceutical research and development, particularly in the area of targeted cancer therapies.
Check Digit Verification of cas no
The CAS Registry Mumber 1456632-40-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,5,6,6,3 and 2 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1456632-40:
(9*1)+(8*4)+(7*5)+(6*6)+(5*6)+(4*3)+(3*2)+(2*4)+(1*0)=168
168 % 10 = 8
So 1456632-40-8 is a valid CAS Registry Number.
1456632-40-8Relevant articles and documents
Potent targeting of the STAT3 protein in brain cancer stem cells: A promising route for treating glioblastoma
Haftchenary, Sina,Luchman, H. Artee,Jouk, Andriana O.,Veloso, Anthony J.,Page, Brent D. G.,Cheng, Xin Ran,Dawson, Sean S.,Grinshtein, Natalie,Shahani, Vijay M.,Kerman, Kagan,Kaplan, David R.,Griffin, Carly,Aman, Ahmed M.,Al-Awar, Rima,Weiss, Samuel,Gunning, Patrick T.
, p. 1102 - 1107 (2013/12/04)
The STAT3 gene is abnormally active in glioblastoma (GBM) and is a critically important mediator of tumor growth and therapeutic resistance in GBM. Thus, for poorly treated brain cancers such as gliomas, astrocytomas, and glioblastomas, which harbor constitutively activated STAT3, a STAT3-targeting therapeutic will be of significant importance. Herein, we report a most potent, small molecule, nonphosphorylated STAT3 inhibitor, 31 (SH-4-54) that strongly binds to STAT3 protein (KD = 300 nM). Inhibitor 31 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations. Moreover, in vivo, 31 exhibited blood-brain barrier permeability, potently controlled glioma tumor growth, and inhibited pSTAT3 in vivo. This work, for the first time, demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.
