jak3-in-6

JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM

JAK3 BTK-IN-6 is a potent dual inhibitor of BTK (IC50: 0.6 nM) and JAK3 (IC50: 0.4 nM).JAK3 BTK-IN-6 exhibits good metabolic stability in human liver microsomes.JAK3 BTK-IN-6 can be used to study blood and immune diseases.

JAK1 TYK2-IN-3 is a selective, potent, orally active dual inhibitor of TYK2 (IC50: 6 nM) and JAK1 (IC50: 37 nM), with selective action on JAK2 (IC50: 140 nM) and JAK3 (IC50: 362 nM). It regulates the expression of TYK2 JAK1-related genes and formation of Th1, Th2, and Th17 cells to exert anti-inflammatory activity.

JAK-IN-25 (compound 19), a potent JAK inhibitor, exhibits IC50 values of 6 nM for TYK2, 21 nM for JAK1, 8 nM for JAK2, and 1051 nM for JAK3. It also demonstrates an IC50 of 28 nM against human whole blood IL-12 (HEB IL-12) and holds potential for cancer research [1].

JAK3-IN-16 (compound 6) is a covalent inhibitor of JAK3.

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.

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. ).