jak-2-in-6

JAK2-IN-6是一种有效的、有选择性的 JAK2抑制剂(ic50为22.86 μg mL),是一种多取代氨基噻唑衍生物。JAK2-IN-6抑制 JAK2酶的活性 ，通过干扰与 JAK2相关的信号通路，从而对 JAK2失调的特定疾病产生治疗作用， 对 JAK1和JAK3不显示出活性。JAK2是一种参与调节细胞生长和分裂的信号通路的蛋白质。JAK2的异常激活与多种疾病有关，包括某些类型的癌症和炎症性疾病。JAK2-IN-6对癌细胞具有抗增殖活性。

Ganoderic acid A 能够抑制 JAK-STAT3信号通路，也能抑制细胞增殖，存活率和 ROS。 它对人骨肉瘤 HOS 和MG-63细胞具有增殖抑制、凋亡和侵袭抑制作用。

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 是一款高效的 JAK HDAC 双靶点抑制剂，能在纳摩尔浓度范围内有效抑制 HDAC3 6 与 JAK1 2。此化合物不仅促进细胞凋亡，还能抑制组蛋白去乙酰化和 STAT3 磷酸化，对血液肿瘤和实体肿瘤细胞展现出了显著的抗增殖效果。