JAK

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1378 Ruxolitinib (INCB018424) <1 mg/mL 61 mg/mL 61 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
S7144 BMS-911543 <1 mg/mL 36 mg/mL 22 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 36 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
S7036 XL019 <1 mg/mL 16 mg/mL <1 mg/mL
S2902 S-Ruxolitinib (INCB018424) 5 mg/mL 61 mg/mL 61 mg/mL
S8004 ZM 39923 HCl <1 mg/mL 30 mg/mL 8 mg/mL
S7650 Peficitinib (ASP015K, JNJ-54781532) <1 mg/mL 65 mg/mL <1 mg/mL
S7605 Filgotinib (GLPG0634) <1 mg/mL 85 mg/mL <1 mg/mL
S7541 Decernotinib (VX-509) <1 mg/mL 78 mg/mL 20 mg/mL
S7259 FLLL32 <1 mg/mL 92 mg/mL 25 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
S8195 Oclacitinib maleate 18 mg/mL 90 mg/mL 90 mg/mL
S7634 Cerdulatinib (PRT062070, PRT2070) <1 mg/mL 43 mg/mL <1 mg/mL
S7119 Go6976 <1 mg/mL 18 mg/mL <1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

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.

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.

S7144

BMS-911543

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.

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.

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.

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.

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.

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.

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.

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.

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.

S2806

CEP-33779

CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.

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.

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.

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.

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.

S7650

Peficitinib (ASP015K, JNJ-54781532)

Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

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.

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.

S7259

FLLL32

FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.

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.

S8195

Oclacitinib maleate

Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.

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.

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.

Catalog No. Information Product Use Citations Product Validations
A5024New

JAK2 Rabbit Recombinant mAb

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