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GNE-2256 (GNE2256) is a potent, selective inhibitor of IRAK4 with biochemical Ki of 1.4 nM.GNE-2256 displays high selectivity in the CEREP panel with off-targets with >50% inhibition are TACR1, HTR2B and ACHE.GNE-2256 is potent in the NanoBRET assay (IC50 = 3.3 nM), the IL-6 human whole blood assay (IC50=190 nM) and the IFNα human whole blood assay (IC50=290 nM).
Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors.
Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib. 12-((4-Bromobutyl)amino)dodecanoic acid can be utilized in PROTAC synthesis.
Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib-induced mechanical hyperalgesia in rats. BI-113823 can be used for the research of chronic inflammatory pain.
Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib-stimulated cAMP production with an IC50 value of 18 nM. L-796778 acetate has anticonvulsant effect.
Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib that can be extracted from C. forskohlii. Deacetylforskolin activates rat adipocyte adenylyl cyclase (IC50 = 20 µM), inhibits glucose transport in rat adipocyte plasma membranes and exhibits antihypertensive activity.
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.
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