JAK

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JAK Inhibitors (25)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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 in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.
  • Nat Cell Biol, 2015, 17(1):57-67
  • J Clin Invest, 2014, 124(12):5263-74
  • Genes Dev, 2012, 26(19):2144-53
S5001 Tofacitinib (CP-690550) Citrate Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 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 in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.
  • Nat Cell Biol, 2015, 17(1):57-67
  • Blood, 2014, 123(10):1516-24
  • Leukemia, 2012, 26(4):708-15
S2736 Fedratinib (SAR302503, TG101348) TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.
  • Blood, 2014, 123(20):3175-84
  • ACS Chem Biol, 2014, 9(5):1160-71
  • Cancer Lett, 2013, 341(2):224-30
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; 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
S7634 Cerdulatinib (PRT062070, PRT2070) Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
S7605 Filgotinib (GLPG0634) Filgotinib (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.
S7119 Go6976 Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
S7137 GLPG0634 analogue GLPG0634 analogue 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.
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 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
  • European Neuropsychopharmacology, 2015, 10.1016/j.euroneuro.2015.04.020
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.
  • Nat Cell Biol, 2015, 17(1):57-67
  • J Clin Invest, 2014, 124(12):5263-74
  • Blood, 2012, 120(19):4093-103
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.
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.
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 in cell-free assays, respectively. Phase 3.
S2407 Curcumol Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities.
S2806 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
  • Biochem Pharmacol, 2014, 91(2):144-56
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
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 in cell-free assays, ~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
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
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.
S2851 Baricitinib (LY3009104, INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.
  • Nat Cell Biol, 2014, 17(1):57-67
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cell line; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.
  • Int J Cancer, 2014, 135(2):282-94
  • J Biol Chem, 2013, 288(36):26167-76
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.
S2179 Gandotinib (LY2784544) Gandotinib (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
S2789 Tofacitinib (CP-690550,Tasocitinib) Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.
  • Nat Cell Biol, 2015, 17(1):57-67
  • Cancer Discov, 2012, 2(7):591-7
  • Genes Dev, 2012, 26(19):2144-53

Hover Mouse over '+' to display IC50

Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1378 Ruxolitinib (INCB018424) <1 mg/mL 61 mg/mL <1 mg/mL
S5001 Tofacitinib (CP-690550) Citrate <1 mg/mL 100 mg/mL <1 mg/mL
S2162 AZD1480 <1 mg/mL 69 mg/mL <1 mg/mL
S2736 Fedratinib (SAR302503, TG101348) <1 mg/mL 100 mg/mL <1 mg/mL
S1134 AT9283 <1 mg/mL 76 mg/mL 38 mg/mL
S7634 Cerdulatinib (PRT062070, PRT2070) <1 mg/mL 43 mg/mL <1 mg/mL
S7605 Filgotinib (GLPG0634) <1 mg/mL 85 mg/mL <1 mg/mL
S7119 Go6976 <1 mg/mL 18 mg/mL <1 mg/mL
S7137 GLPG0634 analogue <1 mg/mL 0.1 mg/mL <1 mg/mL
S1143 AG-490 (Tyrphostin B42) <1 mg/mL 59 mg/mL 6 mg/mL
S2219 Momelotinib (CYT387) <1 mg/mL 74 mg/mL <1 mg/mL
S8004 ZM 39923 HCl <1 mg/mL 30 mg/mL 8 mg/mL
S7036 XL019 <1 mg/mL 16 mg/mL <1 mg/mL
S8057 Pacritinib (SB1518) <1 mg/mL 11 mg/mL <1 mg/mL
S2407 Curcumol <1 mg/mL 47 mg/mL 47 mg/mL
S2806 CEP-33779 <1 mg/mL 93 mg/mL <1 mg/mL
S2214 AZ 960 <1 mg/mL 71 mg/mL 3 mg/mL
S2692 TG101209 <1 mg/mL 102 mg/mL <1 mg/mL
S2686 NVP-BSK805 2HCl 3 mg/mL 113 mg/mL 15 mg/mL
S2902 S-Ruxolitinib (INCB018424) 5 mg/mL 61 mg/mL 61 mg/mL
S2851 Baricitinib (LY3009104, INCB028050) <1 mg/mL 74 mg/mL <1 mg/mL
S2796 WP1066 <1 mg/mL 71 mg/mL <1 mg/mL
S2867 WHI-P154 <1 mg/mL 75 mg/mL <1 mg/mL
S2179 Gandotinib (LY2784544) <1 mg/mL 94 mg/mL 9 mg/mL
S2789 Tofacitinib (CP-690550,Tasocitinib) <1 mg/mL 62 mg/mL <1 mg/mL
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