jak-2-in-6

JAK2-IN-6, a polysubstituted aminothiazole derivative, is a potent and selective inhibitor of JAK2 (ic50 at 22.86 μg mL). Jak2-in-6 inhibits the activity of JAK2 enzymes by interfering with Jak2-related signaling pathways, thereby producing therapeutic effects on the specific disease IN which JAK2 is dysregulated, and does not show activity on JAK1 and JAK3. JAK2 is a protein involved in signaling pathways that regulate cell growth and division. Abnormal activation of JAK2 has been linked to a variety of diseases, including some types of cancer and inflammatory diseases. JAK2-IN-6 has antiproliferative activity against cancer cells.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of myeloma xenografts in mice and enhanced the antitumor activity of relevant agents in combination studies. INCB16562 is a potent JAK1 2 inhibitor and that mitigation of JAK STAT signaling by targeting JAK1 and JAK2 will be beneficial in the treatment of myeloma patients, particularly in combination with other agents. ( source: Neoplasia. 2010 Jan;12(1):28-38. ).

JAK HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1 2 and HDAC3 6 at nanomolar concentrations. This compound exhibits proapoptotic properties, inhibits histone deacetylation, and impedes STAT3 phosphorylation, demonstrating notable antiproliferative activity against various hematological malignancies and solid tumors [1].