118372-34-2

SD-1029 is a Janus kinase 2 (JAK2) inhibitor. It inhibits autophosphorylation of recombinant JAK2 when used at concentrations of 30 and 100 μM and decreases levels of phosphorylated JAK2, but not JAK1 or Src, in MDA-MB-468 and paclitaxel-resistant OVCAR8_TR cells when used at a concentration of 10 μM. SD-1029 (10 μM) decreases levels of phosphorylated STAT3 in MDA-MB-468, MDA-BM-435, OVCAR8_TR, and SKOV3_TR cells and inhibits IL-6-induced nuclear translocation of STAT3 in BHK-21 and U2OS cells. It decreases the viability of and increases levels of cleaved caspase-3 in SNU-387, SNU-398, HepG2, and Huh7 hepatocellular carcinoma cells when used at a concentration of 10 μM. SD-1029 (100 and 1,000 nM) inhibits hepatitis A virus replication in GL37 cells.

SD-1029 is a JAK2/STAT3 inhibitor[1]. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation[2].

STAT3; JAK2

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[1] Zhenfeng Duan, et al. SD-1029 inhibits signal transducer and activator of transcription 3 nuclear translocation. Clin Cancer Res. 2006 Nov 15;12(22):6844-52. DOI:10.1158/1078-0432.CCR-06-1330
[2] Nor Fazila Che Mat, et al. Interleukin-23-induced interleukin-23 receptor subunit expression is mediated by the Janus kinase/signal transducer and activation of transcription pathway in human CD4 T cells. J Interferon Cytokine Res. 2011 Apr;31(4):363-71. DOI:10.1089/jir.2010.0083