JAK2

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.

Protosappanin A is an immunosuppressive ingredient of the medicinal herb Caesalpinia sappan L.

Delgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

LY2784544 is identified as being highly selective for JAK2-V617F and has advanced into human clinical trials for the treatment of several myeloproliferative disorders.

TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity.

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.

TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.