SC99 是一种口服有效选择性STAT3抑制剂，靶向 JAK2-STAT3 途径，抑制血小板活化和聚集，有抗骨髓瘤和抗血栓活性。它结合在 JAK2 的 ATP 结合袋中，抑制 JAK2 和 STAT3 的磷酸化。

SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities

SC99 inhibited the phosphorylation of JAK2 and STAT3 in human platelets but had no effects on the phosphorylation of AKT, p65 or Src, all of which are involved in platelet activation.?SC99 inhibited human platelet aggregation induced by collagen and thrombin in a dose-dependent manner.?SC99 inhibited thrombin-induced P-selectin expression and fibrinogen binding to single platelets.?Moreover, SC99 inhibited platelet spreading on fibrinogen and clot retraction mediated by outside-in signaling.?SC99 inhibited platelet aggregation in mice but it did not significantly prolong the bleeding time.?SC99 inhibited platelet activation and aggregation as a STAT3 inhibitor.?This agent can be developed as a promising treatment for thrombotic disorders.

882290-02-0

C15H8Cl2FN3O

336.15

DMSO:82 mg/mL (243.94 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years