BX-795 is an aminopyrimidine-based, ATP-competitive inhibitor of PDK1, TBK1, and IKKe, with IC50 values of 11 nM, 6 nM, and 41 nM, respectively. [1, 2] BX-795 also potently inhibits ERK8, MNK2, Aurora B, Aurora C, and MARK3. [3] BX-795 inhibits both Thr308-Akt and Thr389-S6K1 phosphorylation at an IC50 of 300 nM. [2]
BX-795 has proven to be a powerful tool in the elucidation of TBK1's and IKKe's role in autophosphorylation events. [1] In particular, it wasfound that BX-795 blocked the autophosphorylation of overexpressed TBK1 and IKKe at Ser172, but did not inhibit endogenous TBK1 and IKKe in response to LPS, poly (I:C), IL-1a). These observations demonstrate that the phosphorylation of Ser172 and activation of TBK1 and IKKe are catalyzed by a distince protein kinase in vivo and that TBK1 and IKKe control a feedback loop that limits their activation to prevent hyperactivation by these enzymes. [1]
Technical information:
| Chemical Formula: | C23H26IN7O2S | |
| CAS #: | 702675-74-9 | |
| Molecular Weight: | 591.47 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | N-(3-(5-iodo-4-(3-(thiophene-2-carboxamido)propylamino)pyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | BX-795, BX795 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Clark 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, 14136-14146. Pubmed ID: 19307177 |
| 2. | Feldman et al., Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J. Biol. Chem. 2005, 280(20), 19867-19874. Pubmed ID: 15772071 |
| 3. | Bain et al., The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007, 408, 297-315. Pubmed ID: 17850214 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
