919486-40-1 Usage
Description
5-PyriMidinecarboxaMide, 2-[[2-(3-chloro-4-hydroxyphenyl)ethyl]aMino]-4-[(phenylMethyl)aMino]-, also known as AS1517499, is a potent STAT6 inhibitor with an IC50 of 21 nM in a reporter assay. It selectively inhibits IL-4-induced Th2 differentiation in mouse spleen T cells without affecting IL-12-induced Th1 differentiation. AS1517499 exhibits various biological activities, including the inhibition of bronchial smooth muscle hyperresponsiveness, IL-13 production, STAT6 phosphorylation, thyroid epithelial cell hyperplasia, and serum levels of thyroid hormones in mouse models of Graves' disease and tumor growth and liver metastasis in a murine orthotopic 4T1 mammary carcinoma model.
Uses
Used in Pharmaceutical Industry:
5-PyriMidinecarboxaMide, 2-[[2-(3-chloro-4-hydroxyphenyl)ethyl]aMino]-4-[(phenylMethyl)aMino]is used as a STAT6 inhibitor for the treatment of various diseases, including Graves' disease and cancer. Its ability to selectively inhibit Th2 differentiation and modulate immune responses makes it a promising candidate for the development of targeted therapies.
Used in Immunology Research:
In the field of immunology, AS1517499 is used as a research tool to study the role of STAT6 in immune cell signaling and differentiation. Its selective inhibition of Th2 differentiation allows researchers to investigate the molecular mechanisms underlying Th1/Th2 balance and the development of allergic and autoimmune diseases.
Used in Drug Discovery:
5-PyriMidinecarboxaMide, 2-[[2-(3-chloro-4-hydroxyphenyl)ethyl]aMino]-4-[(phenylMethyl)aMino]serves as a lead compound in drug discovery efforts aimed at identifying novel STAT6 inhibitors with improved potency, selectivity, and pharmacological properties. Its unique chemical structure and biological activities provide a valuable starting point for the design and optimization of new therapeutic agents targeting STAT6-mediated pathways.
Biochem/physiol Actions
AS1517499 moderately inhibits the expression of RhoA (ras homolog family member A). Overexpression of RhoA protein is associated with allergic bronchial asthma.
Check Digit Verification of cas no
The CAS Registry Mumber 919486-40-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,9,4,8 and 6 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 919486-40:
(8*9)+(7*1)+(6*9)+(5*4)+(4*8)+(3*6)+(2*4)+(1*0)=211
211 % 10 = 1
So 919486-40-1 is a valid CAS Registry Number.
919486-40-1Relevant articles and documents
Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors
Nagashima, Shinya,Yokota, Masaki,Nakai, Ei-ichi,Kuromitsu, Sadao,Ohga, Keiko,Takeuchi, Makoto,Tsukamoto, Shin-ichi,Ohta, Mitsuaki
, p. 1044 - 1055 (2007/10/03)
The STAT6 (signal transducers and activators of transcription 6) protein is activated by interleukin (IL)-4 and IL-13, and plays an important role in T-helper cell 2 (Th2) differentiation. STAT6 might therefore be an excellent therapeutic target for various allergic conditions, including asthma and atopic diseases. We synthesized a series of 2-{[2-(4-hydroxyphenyl)ethyl]amino}pyrimidine-5-carboxamide derivatives and evaluated their STAT6 inhibitory activities. Among these compounds, 4-(benzylamino)-2-{[2-(3-chloro-4-hydroxyphenyl)ethyl]amino}pyrimidine-5-carboxamide (2t, AS1517499) showed potent STAT6 inhibition with an IC50 value of 21 nM, and also inhibited IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM and without influencing T-helper cell 1 (Th1) differentiation induced by IL-12.
