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HS-243 (HS243) is a highly potent, super-selective IRAK-1/4 inhibitor with IC50 of 24/20 nM, respectively.HS-243 shows exquisite potency toward IRAK-1/4 over all other human kinases with only minimal TAK1-inhibiting activity (IC50=0.5 uM).HS-243 binds in the ATP-binding pocket of IRAK-4.HS-243 potently reduces the proinflammatory response of RA cells and macrophages, has distinct cytokine profile from TAK1.HS-243 reduces percentage of survival in pancreatic and breast cancer cell lines.
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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