Cucurbitacin I, Cucumis sativus L. has been found to suppress levels of phosphotyrosine Stat3 (signal transducer and activator of transcription 3) in v-Src-transformed NIH 3T3 cells.
SD 1008 is reported to be a JAK2/STAT3 signaling pathway inhibitor which additionally inhibits Src. SD 1008 is noted to induce apoptosis in cell lines that express constitutively active tyrosine-phosphorylated STAT3.
TCS 21311 is a potent JAK3 inhibitor (IC50 = 8 nM). TCS 21311 is selective for JAK3 over JAK1, JAK2 and Tyk 2 (IC50 values are 1017, 2550 and 8055 nM respectively).
NSC 33994 is novel inhibitor of JAK2 tyrosine kinase (Janus kinase 2 ). Janus kinase 2 (JAK2) plays a crucial role in the pathomechanism of myeloproliferative disorders and hematological malignancies.
LY2784544 is identified as being highly selective for JAK2-V617F and has advanced into human clinical trials for the treatment of several myeloproliferative disorders.
GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
