JAK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

JAK Products

All (44) JAK Inhibitors (44) New JAK Products

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.	Cancer Discov, 2019, 9(1):34-45 Cell Stem Cell, 2019, 25(1):69-86 Cancer Cell, 2019, 36(2):179-193	STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.
S5001	Tofacitinib (CP-690550) Citrate Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively.	J Immunol, 2019, 202(10):2924-2944 Inflamm Bowel Dis, 2019, 25(4):647-660 Drug Metab Dispos, 2018, 46(2):131-140	CP-690550 reduced the severity of ischemic damage. (A) CP-690550 (10 μM) suppressed IL-17 production by cdT cells and activated memory T cells. cdT cells and CD4+ CD44+ memory T cells isolated from C5BL6J mice through flow cytometry were stimulated for 24 h with plate-bound monoclonal antibodies to CD3 (2 ng/ml) and CD28 (1 ng/ml) in the presence or absence of IL-23 (25 ng/ml). IL-17A production and IL-17A expression level were measured by quantitative RT-PCR (a) and ELISA (b). (B) CBF reduction after brain ischemia. (C) Time-dependent changes in neurological score. *p < 0.05. (D) Infarct volume as visualized through TTC staining on day 3 in CP-690550 (CP)- and vehicle-treated mice.
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.	Cell Stem Cell, 2019, 25(1):69-86 Cancers (Basel), 2019, 11(1) Am J Physiol Lung Cell Mol Physiol, 2019, 316(3):L487-L497	HEL cells were treated for 3 hours with the indicated concentrations of AZD1480. AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar concentrations in intact cells.
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.	FASEB J, 2019, 10.1096/fj.201900215RR Cancer Cell, 2018, 34(2):315-330 Proc Natl Acad Sci U S A, 2018, 115(46):11766-11771	Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
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.	Mol Cancer Ther, 2016, 15(2):334-42 Gastric Cancer, 2016, 19(1):53-62 Cancer Lett, 2014, 354(1):68-76	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
S8162^New	Upadacitinib (ABT-494) Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.
S6524^New	NSC 42834 NSC42834 is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM.
S6521^New	WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM.
S8684^New	Selective JAK3 inhibitor 1 Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
S8804^New	PF-06700841 PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
S8765^New	PF-04965842 PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.
S5917^New	Solcitinib Solcitinib is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.
S5902^New	1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-Hexabromocyclohexane is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range.	Cell Tissue Res, 2016, 364(2):395-404
S5903^New	JANEX-1 JANEX-1 is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM).
S5904^New	WHI-P97 WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays.
S5754^New	Baricitinib phosphate Baricitinib phosphate 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.	Arthritis Rheumatol, 2019, 71(1):50-62
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.	Int Immunopharmacol, 2019, 73:482-490 Oncol Rep, 2019, 41(3):1883-1892 Transl Oncol, 2018, 11(4):971-978	IL-6- supported INA-6 cells were treated with the JAK inhibitors ruxolitinib (Rux; 10 nM) or CYT387 (CYT; 50 nM) for 1 hour and assessed for inhibition of STAT3 phosphorylation by immunoblotting.
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.	J Thromb Haemost, 2019, 10.1111/jth.14525 Pharmacol Res, 2019, 143:73-85 Immunotherapy, 2019, 11(6):483-496	TRAP-positive multinucleated cell differentiation depends on JAK and is inhibited by tofacitinib in vitro. Effect of tofacitinib on the differentiation of TRAP-positive multi-nucleated cells in vitro (n =3 wells/experiment). Original magnification x 100.
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.	Haematologica, 2019, 10.3324/haematol.2018.203430 Redox Biol, 2019, 24:101189 Glia, 2019, 67(2):321-331	Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.
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.	Int Immunopharmacol, 2018, 54:354-365 Leukemia, 2014, 28(7):1519-28 ACS Chem Biol, 2014, 9(5):1160-71	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
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.	J Thromb Haemost, 2019, 10.1111/jth.14525 Biochem Biophys Res Commun, 2018, 498(1):164-170 Cell Chem Biol, 2017, 24(7):858-869	HEL cells were treated for 3 hours with the indicated concentrations of LY2784544. LY2784544 inhibits Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells.
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.	J Biol Chem, 2015, 290(39):23553-62 Cancer Lett, 2013, 341(2):224-30 PLoS One, 2013, 8(5):e63301	Determination of the kynurenine production in HFF cells after IDO induction by IFN-γ (100 U/mL). The cells were incubated for 72 h under normoxia (20% O2) or hypoxia (1% O2) and treated with different amounts of the JAK2 inhibitor BSK805 (0-2 uM).
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.	Nephron, 2019, 10.1159/000499506 Arthritis Rheumatol, 2018, doi.org/10.1002/art.40670 Sci Rep, 2018, 8(1):15645	bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.
S2214	AZ 960 AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and K_i of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.	Cytokine, 2019, 113:238-247 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.	Sci Rep, 2018, 8(1):15645 Biosci Rep, 2017, 37(4) Anticancer Res, 2017, 37(12):6761-6769	Potentiation of the antitumor effects of vincristine by CEP-33779 in a KBv200 cell xenograft model in nude mice. (A) The changes in tumor volume with time after tumor cell implantation. (B) The photograph of tumor size was taken on the 21st day after implantation. The various treatments were as follows: (a) Control (vehicle alone); (b) Vincristine (q2d x 6, ip, 0.2 mg/kg); (c) CEP-33779 (q2d x 6, p.o, 30 mg/kg) and (d) Vincristine (q2d x 6, ip, 0.2 mg/kg) plus CEP-33779 (q2d ?6, p.o, 30 mg/kg, given an hour before Vincristine administration).
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.	Exp Cell Res, 2019, 378(1):11-20 Clin Cancer Res, 2016, 22(24):6118-6128	Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
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.	Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8 Oncol Rep, 2017, 37(1):66-76	Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.
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.	Anticancer Res, 2017, 37(12):6761-6769
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.	Blood Cancer J, 2017, 7(6):e572 Nature, 2017, 548(7668):471-475 Sci Rep, 2016, 6:28473
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.	Cancer Sci, 2018, 109(12):3726-3736
S8538	PF-06651600 PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.
S5243	Ruxolitinib Phosphate Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.	Clin Breast Cancer, 2018, 18(5):e1205-e1215 Leuk Res, 2018, 74:57-63 Cytokine, 2017, 90:73-79
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.	Cancer Immunol Res, 2019, 7(5):813-827 Arthritis Rheumatol, 2018, 70(12):2057-2066 J Immunol, 2018, 200(8):2603-2614	Confocal microscopy showing BAFF in ductal epithelial structures within SG organoids from patients with sicca (Sc) or primary Sjögren's syndrome (SS). Nuclei were stained with DAPI (blue). Original magnification × 100.
S7541	Decernotinib (VX-509) Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with K_i of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
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.	J Pathol, 2019, 10.1002/path.5280 Cancer Sci, 2018, 109(12):3726-3736
S7259	FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.	Exp Ther Med, 2017, 14(4):3926-3934 Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011 Cancer Sci, 2016, 107(7):944-54	Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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.		Western blots showing the expression of γ-globin after treatments with (F) GLPG0634.
S8195	Oclacitinib maleate Oclacitinib(PF 03394197) 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. It does 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.	Int J Oncol, 2018, 53(4):1681-1690 Diabetologia, 2018, 61(3):636-640 J Immunol, 2017, 198(12):4596-4606
S8541	FM-381 FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.
S7812	Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
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.	Acta Physiol, 2018, 223(3):e13055 Biochim Biophys Acta Mol Basis Dis, 2018, 1864(9 Pt B):2957-2971 J Biol Chem, 2018, 10.1074/jbc.RA118.002191	Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.

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.	Cancer Discov, 2019, 9(1):34-45 Cell Stem Cell, 2019, 25(1):69-86 Cancer Cell, 2019, 36(2):179-193	STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.
S5001	Tofacitinib (CP-690550) Citrate Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively.	J Immunol, 2019, 202(10):2924-2944 Inflamm Bowel Dis, 2019, 25(4):647-660 Drug Metab Dispos, 2018, 46(2):131-140	CP-690550 reduced the severity of ischemic damage. (A) CP-690550 (10 μM) suppressed IL-17 production by cdT cells and activated memory T cells. cdT cells and CD4+ CD44+ memory T cells isolated from C5BL6J mice through flow cytometry were stimulated for 24 h with plate-bound monoclonal antibodies to CD3 (2 ng/ml) and CD28 (1 ng/ml) in the presence or absence of IL-23 (25 ng/ml). IL-17A production and IL-17A expression level were measured by quantitative RT-PCR (a) and ELISA (b). (B) CBF reduction after brain ischemia. (C) Time-dependent changes in neurological score. *p < 0.05. (D) Infarct volume as visualized through TTC staining on day 3 in CP-690550 (CP)- and vehicle-treated mice.
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.	Cell Stem Cell, 2019, 25(1):69-86 Cancers (Basel), 2019, 11(1) Am J Physiol Lung Cell Mol Physiol, 2019, 316(3):L487-L497	HEL cells were treated for 3 hours with the indicated concentrations of AZD1480. AZD1480 inhibits Jak2-V617F mediated signal transduction at micromolar concentrations in intact cells.
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.	FASEB J, 2019, 10.1096/fj.201900215RR Cancer Cell, 2018, 34(2):315-330 Proc Natl Acad Sci U S A, 2018, 115(46):11766-11771	Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
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.	Mol Cancer Ther, 2016, 15(2):334-42 Gastric Cancer, 2016, 19(1):53-62 Cancer Lett, 2014, 354(1):68-76	HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
S8162^New	Upadacitinib (ABT-494) Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.
S6524^New	NSC 42834 NSC42834 is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM.
S6521^New	WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM.
S8684^New	Selective JAK3 inhibitor 1 Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
S8804^New	PF-06700841 PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
S8765^New	PF-04965842 PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.
S5917^New	Solcitinib Solcitinib is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.
S5902^New	1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-Hexabromocyclohexane is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range.	Cell Tissue Res, 2016, 364(2):395-404
S5903^New	JANEX-1 JANEX-1 is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM).
S5904^New	WHI-P97 WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays.
S5754^New	Baricitinib phosphate Baricitinib phosphate 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.	Arthritis Rheumatol, 2019, 71(1):50-62
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.	Int Immunopharmacol, 2019, 73:482-490 Oncol Rep, 2019, 41(3):1883-1892 Transl Oncol, 2018, 11(4):971-978	IL-6- supported INA-6 cells were treated with the JAK inhibitors ruxolitinib (Rux; 10 nM) or CYT387 (CYT; 50 nM) for 1 hour and assessed for inhibition of STAT3 phosphorylation by immunoblotting.
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.	J Thromb Haemost, 2019, 10.1111/jth.14525 Pharmacol Res, 2019, 143:73-85 Immunotherapy, 2019, 11(6):483-496	TRAP-positive multinucleated cell differentiation depends on JAK and is inhibited by tofacitinib in vitro. Effect of tofacitinib on the differentiation of TRAP-positive multi-nucleated cells in vitro (n =3 wells/experiment). Original magnification x 100.
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.	Haematologica, 2019, 10.3324/haematol.2018.203430 Redox Biol, 2019, 24:101189 Glia, 2019, 67(2):321-331	Effects of selective STAT3 inhibitors on adherent glioma CSCs. Cells were treated with WP1066 (50 uM for 2 h) or vehicle, and colocalization of STAT3 and p65 was determined by immunostaining.
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.	Int Immunopharmacol, 2018, 54:354-365 Leukemia, 2014, 28(7):1519-28 ACS Chem Biol, 2014, 9(5):1160-71	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
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.	J Thromb Haemost, 2019, 10.1111/jth.14525 Biochem Biophys Res Commun, 2018, 498(1):164-170 Cell Chem Biol, 2017, 24(7):858-869	HEL cells were treated for 3 hours with the indicated concentrations of LY2784544. LY2784544 inhibits Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells.
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.	J Biol Chem, 2015, 290(39):23553-62 Cancer Lett, 2013, 341(2):224-30 PLoS One, 2013, 8(5):e63301	Determination of the kynurenine production in HFF cells after IDO induction by IFN-γ (100 U/mL). The cells were incubated for 72 h under normoxia (20% O2) or hypoxia (1% O2) and treated with different amounts of the JAK2 inhibitor BSK805 (0-2 uM).
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.	Nephron, 2019, 10.1159/000499506 Arthritis Rheumatol, 2018, doi.org/10.1002/art.40670 Sci Rep, 2018, 8(1):15645	bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.
S2214	AZ 960 AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and K_i of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3.	Cytokine, 2019, 113:238-247 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.	Sci Rep, 2018, 8(1):15645 Biosci Rep, 2017, 37(4) Anticancer Res, 2017, 37(12):6761-6769	Potentiation of the antitumor effects of vincristine by CEP-33779 in a KBv200 cell xenograft model in nude mice. (A) The changes in tumor volume with time after tumor cell implantation. (B) The photograph of tumor size was taken on the 21st day after implantation. The various treatments were as follows: (a) Control (vehicle alone); (b) Vincristine (q2d x 6, ip, 0.2 mg/kg); (c) CEP-33779 (q2d x 6, p.o, 30 mg/kg) and (d) Vincristine (q2d x 6, ip, 0.2 mg/kg) plus CEP-33779 (q2d ?6, p.o, 30 mg/kg, given an hour before Vincristine administration).
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.	Exp Cell Res, 2019, 378(1):11-20 Clin Cancer Res, 2016, 22(24):6118-6128	Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
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.	Biol Open, 2018, 7(1) J Mol Med, 2018, 10.1007/s00109-018-1724-8 Oncol Rep, 2017, 37(1):66-76	Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.
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.	Anticancer Res, 2017, 37(12):6761-6769
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.	Blood Cancer J, 2017, 7(6):e572 Nature, 2017, 548(7668):471-475 Sci Rep, 2016, 6:28473
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.	Cancer Sci, 2018, 109(12):3726-3736
S8538	PF-06651600 PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.
S5243	Ruxolitinib Phosphate Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.	Clin Breast Cancer, 2018, 18(5):e1205-e1215 Leuk Res, 2018, 74:57-63 Cytokine, 2017, 90:73-79
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.	Cancer Immunol Res, 2019, 7(5):813-827 Arthritis Rheumatol, 2018, 70(12):2057-2066 J Immunol, 2018, 200(8):2603-2614	Confocal microscopy showing BAFF in ductal epithelial structures within SG organoids from patients with sicca (Sc) or primary Sjögren's syndrome (SS). Nuclei were stained with DAPI (blue). Original magnification × 100.
S7541	Decernotinib (VX-509) Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with K_i of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
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.	J Pathol, 2019, 10.1002/path.5280 Cancer Sci, 2018, 109(12):3726-3736
S7259	FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM.	Exp Ther Med, 2017, 14(4):3926-3934 Eur Rev Med Pharmacol Sci, 2017, 21(13):3005-3011 Cancer Sci, 2016, 107(7):944-54	Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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.		Western blots showing the expression of γ-globin after treatments with (F) GLPG0634.
S8195	Oclacitinib maleate Oclacitinib(PF 03394197) 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. It does 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.	Int J Oncol, 2018, 53(4):1681-1690 Diabetologia, 2018, 61(3):636-640 J Immunol, 2017, 198(12):4596-4606
S8541	FM-381 FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.
S7812	Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
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.	Acta Physiol, 2018, 223(3):e13055 Biochim Biophys Acta Mol Basis Dis, 2018, 1864(9 Pt B):2957-2971 J Biol Chem, 2018, 10.1074/jbc.RA118.002191	Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.

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