Cat. No. Name Size Price Add Cart
KI3724BX79510 mg$127
BX79525 mg$272
BX79550 mg$485
BX795100 mg$825

Chemical Characteristic

Product NameBX795
CAS No.702675-74-9
Molecular Weight 591.47
FormulaC23H26IN7O2S
Chemical NameN-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
SmilesN1(CCCC1)C(=O)Nc1cc(ccc1)Nc1nc(c(cn1)I)NCCCNC(=O)c1cccs1
Chemical Structure

Biological activities

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively [1]. BX795 is a potent and relatively specific inhibitor of TBK1 and IKKepsilon, blocked the phosphorylation, nuclear translocation, and transcriptional activity of interferon regulatory factor 3 and so that 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. In vitro, BX795 can be used by 1?M in RAW 264.7 [2].

References

[1] Feldman RI, Wu JM, Polokoff MA, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005, 280(20):19867-19874.
[2] Clark K, Plater L, Peggie M, et al. 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. J Biol Chem. 2009, 284(21):14136-14146.

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