BX795 - CAS 702675-74-9
Catalog number: B0084-194478
Category: Inhibitor
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BX795 is a potent and selective inhibitor of PDK1, IKKε and TBK1, which regulates the production of Type 1 interferons during bacterial and viral infection. BX795 blocks the phosphorylation, nuclear translocation, and transcriptional activity of interferon regulatory factor 3 and the production of interferon-β in macrophages stimulated with poly(I:C) or lipopolysaccharide (LPS). BX795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1.
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B0084-194478 25 mg $189 In stock
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Brife Description:
PDK1/IKKε/TBK1 inhibitor
BX-795; BX 795; BX795. N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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1.An off-target effect of BX795 blocks herpes simplex virus type 1 infection of the eye.
Jaishankar D;Yakoub AM;Yadavalli T;Agelidis A;Thakkar N;Hadigal S;Ames J;Shukla D Sci Transl Med. 2018 Feb 14;10(428). pii: eaan5861. doi: 10.1126/scitranslmed.aan5861.
Herpes simplex virus type 1 (HSV-1) causes recurrent mucocutaneous lesions in the eye that may advance to corneal blindness. Nucleoside analogs exemplified by acyclovir (ACV) form the primary class of antiherpetic drugs, but this class suffers limitations due to the emergence of viral resistance and other side effects. While studying the molecular basis of ocular HSV-1 infection, we observed that BX795, a commonly used inhibitor of TANK-binding kinase 1 (TBK1), strongly suppressed infection by multiple strains of HSV-1 in transformed and primary human cells, cultured human and animal corneas, and a murine model of ocular infection. Our investigations revealed that the antiviral activity of BX795 relies on targeting Akt phosphorylation in infected cells, leading to the blockage of viral protein synthesis. This small-molecule inhibitor, which was also effective against an ACV-resistant HSV-1 strain, shows promise as an alternative to existing drugs and as an effective topical therapy for ocular herpes infection. Collectively, our results obtained using multiple infection models and virus strains establish BX795 as a promising lead compound for broad-spectrum antiviral applications in humans.
2.TBK1 inhibitors: a review of patent literature (2011 - 2014).
Yu T;Yang Y;Yin DQ;Hong S;Son YJ;Kim JH;Cho JY Expert Opin Ther Pat. 2015;25(12):1385-96. doi: 10.1517/13543776.2015.1081168. Epub 2015 Aug 19.
INTRODUCTION: ;TANK-binding kinase 1 (TBK1) is a noncanonical IκB kinase family member that regulates the innate immune response. Misregulation of TBK1 activity can promote inflammatory disorders and oncogenesis; therefore, TBK1 inhibitors are considered a promising therapy for inflammation and cancer.;AREAS COVERED: ;In this review, the authors provide information on the role of TBK1 in human health and on recently developed inhibitors from patents granted from 2011 to 2014. The reader will gain an understanding of the mechanisms of TBK1 function as well as the structure and biological activity of recently developed TBK1 inhibitors. Google and NCBI search engines were used to find relevant patents and clinical information using "TBK1 inhibitor" as the search term.;EXPERT OPINION: ;The role of TBK1 in various diseases has prompted the further investigation of significant targets. Although research on TBK1 inhibitors has increased over the last few years, only a few inhibitors of this kinase have been identified. In addition, almost all of the chemical inhibitors are modified from different scaffolds and/or chemotypes of pyrimidine. Specifically, compound BX795 is the representative one, which was first patented as a potent TBK1 inhibitor.
3.Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation.
Clark K;Plater L;Peggie M;Cohen P J Biol Chem. 2009 May 22;284(21):14136-46. doi: 10.1074/jbc.M109.000414. Epub 2009 Mar 22.
TANK-binding kinase 1 (TBK1) and IkappaB kinase epsilon (IKKepsilon) regulate the production of Type 1 interferons during bacterial and viral infection, but the lack of useful pharmacological inhibitors has hampered progress in identifying additional physiological roles of these protein kinases and how they are regulated. Here we demonstrate that BX795, a potent and relatively specific inhibitor of TBK1 and IKKepsilon, blocked the phosphorylation, nuclear translocation, and transcriptional activity of interferon regulatory factor 3 and, hence, the production of interferon-beta in macrophages stimulated with poly(I:C) or lipopolysaccharide (LPS). In contrast, BX795 had no effect on the canonical NFkappaB signaling pathway. Although BX795 blocked the autophosphorylation of overexpressed TBK1 and IKKepsilon at Ser-172 and, hence, the autoactivation of these protein kinases, it did not inhibit the phosphorylation of endogenous TBK1 and IKKepsilon at Ser-172 in response to LPS, poly(I:C), interleukin-1alpha (IL-1alpha), or tumor necrosis factor alpha and actually enhanced the LPS, poly(I:C), and IL-1alpha-stimulated phosphorylation of this residue. These results demonstrate that the phosphorylation of Ser-172 and the activation of TBK1 and IKKepsilon are catalyzed by a distinct protein kinase(s) in vivo and that TBK1 and IKKepsilon control a feedback loop that limits their activation by LPS, poly(I:C) and IL-1alpha (but not tumor necrosis factor alpha) to prevent the hyperactivation of these enzymes.
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CAS 702675-74-9 BX795

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