JAK

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JAK Inhibitors (21)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1378 Ruxolitinib (INCB018424) INCB018424 is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
  • Genes Dev, 2013, 26(19):2144-53
  • Blood, 2014, 123(24):3832-42
  • J Immunol, 2012, 189(6):2784-92
S5001 Tofacitinib (CP-690550) Citrate Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
  • J Exp Med, 2012, 209(2):259-73
  • Blood, 2011, 118(14):3911-21
  • Blood, 2014, 124(5):761-70
S2162 AZD1480 AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.
  • Leukemia, 2012, 26(4):708-15
  • Mol Cell Proteomics, 2012, 11(6):M112.017764
  • Cancer Lett, 2013, 341(2):224-30
S2736 Fedratinib (SAR302503, TG101348) TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.
  • ACS Chem Biol, 2014, 10.1021/cb500072z
  • Cancer Lett, 2013, 341(2):224-30
  • PLoS One, 2013, 8(8): e74676
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 2.
  • Cell Stem Cell, 2012, 11(2):179-94
  • Cancer Res, 2013, 73(20):6310-22
  • Cancer Lett, 2013, 341(2):224-30
S7137 GLPG0634 GLPG0634 is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
S8057 Pacritinib (SB1518) Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM, respectively. Phase 3.
S7036 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1.
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
  • Clin Cancer Res, 2013, 19(17):4697-705
  • Mol Cancer, 2014, 13:176
  • Carcinogenesis, 2014, 35(4):795-806
S2219 Momelotinib (CYT387) Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.
  • Blood, 2012, 120(19):4093-103
  • Cancer Lett, 2013, 341(2):224-30
S8004 ZM 39923 HCl ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.
S2179 LY2784544 LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
  • Cancer Lett, 2013, 341(2):224-30
S2214 AZ 960 AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.
  • Cancer Lett, 2013, 341(2):224-30
S2686 NVP-BSK805 2HCl NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2.
  • Cancer Lett, 2013, 341(2):224-30
  • PLoS One, 2013, 8(5):e63301
S2692 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.
  • Leukemia, 2014, 28(7):1519-28
  • ACS Chem Biol, 2014, 9(5):1160-71
  • Cancer Lett, 2013, 341(2):224-30
S2789 Tofacitinib (CP-690550,Tasocitinib) Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
  • Cancer Discov, 2012, 2(7):591-7
  • Genes Dev, 2012, 26(19):2144-53
  • Blood, 2012, 120(4):709-19
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.
  • Int J Cancer, 2013, 135(2):282-94
  • J Biol Chem, 2013, 288(36):26167-76
S2806 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
S2851 Baricitinib (LY3009104, INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.
S2867 WHI-P154 WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
S2902 S-Ruxolitinib (INCB018424) S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3.