JAK

JAK Inhibitors (28)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1378 Ruxolitinib (INCB018424) Ruxolitinib (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 Med, 2015, 10.1038/nm.4013
  • Cancer Cell, 2015, 28(1):29-41
  • Cancer Cell, 2015, 28(1):29-41
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.
  • Nat Cell Biol, 2015, 17(1):57-67
  • Cancer Discov, 2012, 2(7):591-7
  • Genes Dev, 2012, 26(19):2144-53
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) Fedratinib (SAR302503, TG101348) 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.
  • Cell, 2015, 162(2):441-51
  • Blood, 2014, 123(20):3175-84
  • 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
S7541 Decernotinib (VX-509) Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
S7650 Peficitinb (ASP015K, JNJ-54781532) Peficitinb (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
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
  • Cancer Lett, 2015, 359(2):335-43
  • Cancer Lett, 2013, 341(2):224-30
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
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.
  • Mol Syst Biol, 2015, 11(3):797
  • Genes Dev, 2012, 26(19):2144-53
  • J Exp Med, 2012, 209(2):259-73
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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, 2014, 135(2):282-94
  • Exp Neurol, 2015, 271:445-56
  • J Biol Chem, 2013, 288(36):26167-76
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
  • Cancer Lett, 2013, 341(2):224-30
  • ACS Chem Biol, 2014, 9(5):1160-71
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
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
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
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
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
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.
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.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
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.
S2407 Curcumol Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities.
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.
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.
  • Cell Signal, 2016, 28(9):1422-31
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.
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.
S7259 FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.
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All JAK Products

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
S7541 Decernotinib (VX-509) <1 mg/mL 78 mg/mL 20 mg/mL
S7650 Peficitinb (ASP015K, JNJ-54781532) <1 mg/mL 65 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
S2789 Tofacitinib (CP-690550,Tasocitinib) <1 mg/mL 62 mg/mL <1 mg/mL
S2796 WP1066 <1 mg/mL 71 mg/mL <1 mg/mL
S2692 TG101209 <1 mg/mL 102 mg/mL <1 mg/mL
S2179 Gandotinib (LY2784544) <1 mg/mL 94 mg/mL 9 mg/mL
S2686 NVP-BSK805 2HCl 3 mg/mL 113 mg/mL 15 mg/mL
S2851 Baricitinib (LY3009104, INCB028050) <1 mg/mL 74 mg/mL <1 mg/mL
S2214 AZ 960 <1 mg/mL 71 mg/mL 3 mg/mL
S2806 CEP-33779 <1 mg/mL 93 mg/mL <1 mg/mL
S8057 Pacritinib (SB1518) <1 mg/mL 11 mg/mL <1 mg/mL
S2867 WHI-P154 <1 mg/mL 75 mg/mL <1 mg/mL
S2902 S-Ruxolitinib (INCB018424) 5 mg/mL 61 mg/mL 61 mg/mL
S7036 XL019 <1 mg/mL 16 mg/mL <1 mg/mL
S8004 ZM 39923 HCl <1 mg/mL 30 mg/mL 8 mg/mL
S2407 Curcumol <1 mg/mL 47 mg/mL 47 mg/mL
S7137 GLPG0634 analogue <1 mg/mL 0.1 mg/mL <1 mg/mL
S7119 Go6976 <1 mg/mL 18 mg/mL <1 mg/mL
S7605 Filgotinib (GLPG0634) <1 mg/mL 85 mg/mL <1 mg/mL
S7634 Cerdulatinib (PRT062070, PRT2070) <1 mg/mL 43 mg/mL <1 mg/mL
S7259 FLLL32 <1 mg/mL 92 mg/mL 25 mg/mL
Tags: JAK inhibition | JAK pathway | JAK/stat pathway | JAK drugs | JAK activation | JAK assay | JAK cancer | JAK phosphorylation | JAK2 inhibitors clinical trials | JAK inhibitors in development | JAK2 inhibitor drug | JAK inhibitor review
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