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JAK Signaling Pathway Map

JAK Signaling Pathways

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Catalog No. Product Name Information Product Use Citations Product Validations
E0011 Linderalactone Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
E0700New cucurbitacin E Cucurbitacin E (α-Elaterin; α-Elaterine), a tetracyclic triterpene derived from the climbing stem of Cucumic melo L, is an inhibitor of JAK2 and STAT3.
E0769New Ginsenoside Rh4 Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways.
E0793New G5-7 G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.
E2821New RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
S0374 GDC046 GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).
S0391 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
S0437 SAR-20347 SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling.
S0871 Gusacitinib (ASN-002) Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
S0981 BD750 BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively.
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, Abl1(T315I). Phase 2.
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
Sci Rep, 2022, 12(1):7
Mol Syst Biol, 2021, 17(9):e10426
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42, Zinc02557947) 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.
J Exp Med, 2022, 219(4)e20211498
Cancer Lett, 2022, 544:215812
J Headache Pain, 2022, 23(1):25
S1349 SC99 SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway by docking into the ATP-binding pocket of JAK2, also inhibits phosphorylation of JAK2and STAT3 with no effects on the other kinases associated with STAT3 signaling.
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. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Blood, 2022, blood.2021014304
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Blood, 2022, blood.2021012366
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Mol Neurodegener, 2022, 17(1):7
Int J Mol Sci, 2022, 23(8)4077
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.
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
Sci Rep, 2022, 12(1):7
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. AZ 960 induces apoptosis and growth arrest.
Cancers (Basel), 2022, 14(6)1575
BMC Cancer, 2021, 21(1):1213
Carcinogenesis, 2020, 41(7):993-1004
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Stem Cell, 2021, S1934-5909(21)00344-1
Cancer Res, 2021, canres.0955.2021
S2407 Curcumol Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities.
J Ethnopharmacol, 2021, 280:114413
Cell Prolif, 2020, 53(3):e12762
Phytother Res, 2020, 10.1002/ptr.6968
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.
Int J Mol Sci, 2022, 23(9)4597
Sci Rep, 2022, 12(1):7
Elife, 2021, 10e60646
S2692 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-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.
EBioMedicine, 2022, 78:103963
FASEB J, 2022, 36(6):e22336
Sci Rep, 2022, 12(1):7
S2736 Fedratinib (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. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
J Immunother Cancer, 2022, 10(1)e003766
Int J Mol Sci, 2022, 23(9)4597
Int J Mol Sci, 2022, 23(4)2019
S2789 Tofacitinib (CP-690550) 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. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis.
Blood, 2022, blood.2021012366
J Clin Invest, 2022, 132(11)e139298
J Immunother Cancer, 2022, 10(1)e003766
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. WP1066 induces apoptosis. Phase 1.
Cell Biosci, 2022, 12(1):43
Commun Biol, 2022, 5(1):105
Neurochem Res, 2022, 10.1007/s11064-022-03655-4
S2806 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
Int J Mol Sci, 2022, 23(9)4597
Sci Rep, 2022, 12(1):7
Nat Med, 2020, 10.1038/s41591-020-0926-0
S2851 Baricitinib (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. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
Blood, 2022, blood.2021012366
NPJ Digit Med, 2022, 5(1):83
J Immunother Cancer, 2022, 10(1)e003766
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.
Sci Rep, 2022, 12(1):7
Am J Transplant, 2021, 21(7):2360-2371
J Med Chem, 2020, 31
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.
Nat Commun, 2021, 12(1):2346
PLoS Pathog, 2021, 17(12):e1010174
Nat Med, 2020, 10.1038/s41591-020-0926-0
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S3566 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) 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 inhibits19 other tested kinases with IC50 less than 200 nM.
S5001 Tofacitinib (CP-690550) Citrate Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity.
Blood, 2022, blood.2021012366
J Clin Invest, 2022, 132(11)e139298
J Control Release, 2022, S0168-3659(22)00163-8
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib 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. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Cancer Cell, 2022, S1535-6108(21)00662-0
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Blood, 2022, blood.2021012366
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S5588 Creatine Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue.Creatine can inhibits the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression.
Cancer Cell, 2021, S1535-6108(21)00445-1
Histochem Cell Biol, 2021, 156(3):227-237
S5754 Baricitinib phosphate Baricitinib phosphate (INCB-028050, LY-3009104) 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. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19.
Arthritis Res Ther, 2022, 24(1):43
Immunol Res, 2022, 10.1007/s12026-022-09261-4
J Immunother Cancer, 2021, 9(6)e002305
S5902 1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-Hexabromocyclohexane (NSC7908) 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 JANEX-1 JANEX-1 (WHI-P131) 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).
Exp Biol Med (Maywood), 2020, 1535370220942470
S5904 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.
J Med Chem, 2020, 31
S5917 Solcitinib Solcitinib (GLPG0778, GSK2586184) 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.
Cancer Lett, 2021, 510:37-47
bioRxiv, 2021, N/A
Front Immunol, 2020, 11:1303
S6521 WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM.
S6524 NSC 42834 NSC42834 (JAK2 Inhibitor V, Z3) is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM.
S6789 JAK Inhibitor I (Pyridone 6) JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
S7002New Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
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.
Sci Rep, 2022, 12(1):7
Molecules, 2021, 26(3)606
J Med Chem, 2020, 31
S7119 Go6976 Go6976 (PD406976) 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 Biosci, 2022, 12(1):43
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Biochimie, 2021, 184:8-17
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.
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.
NPJ Precis Oncol, 2021, 5(1):75
Oncogene, 2019, 38(9):1477-1488
J Pathol, 2019, 10.1002/path.5280
S7198 BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cell Rep, 2022, 38(12):110538
J Cell Physiol, 2022, 10.1002/jcp.30724
S7259 FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
Syst Biol Reprod Med, 2022, 1-15
Pathol Oncol Res, 2022, 28:1610273
Int Immunopharmacol, 2021, 92:107304
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.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Pharmacol Res, 2022, 182:106318
Sci Rep, 2022, 12(1):7
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.
Haematologica, 2022, 10.3324/haematol.2021.279848
Sci Rep, 2022, 12(1):7
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7634 Cerdulatinib (PRT062070) hydrochloride Cerdulatinib (PRT-062070, PRT2070) hydrochloride 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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Lett, 2021, 512:28-37
S7650 Peficitinib (ASP015K) Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
S7812 Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
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.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
Int J Biol Sci, 2019, 15(9):1882-1891
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.
Clin Transl Med, 2022, 12(6):e894
J Innate Immun, 2022, 1-11
Sci Rep, 2022, 12(1):7
S8152 Cucurbitacin I

Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3.

S8162 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.
J Dermatol Sci, 2022, S0923-1811(22)00092-5
J Clin Med, 2021, 10(7)1431
Platelets, 2021, 1-12
S8195 Oclacitinib maleate Oclacitinib maleate (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.
Sci Rep, 2022, 12(1):7
Platelets, 2021, 1-12
Carcinogenesis, 2020, 41(7):993-1004
S8538 Ritlecitinib (PF-06651600) Ritlecitinib (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.
Drug Des Devel Ther, 2022, 16:363-374
Front Oncol, 2021, 11:807200
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.
Commun Biol, 2020, 3:8
S8684 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.
S8765 Abrocitinib (PF-04965842) Abrocitinib (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.
Int J Med Sci, 2020, 18;17(5):609-619
Cell Death Dis, 2019, 10(4):319
Biochem Biophys Res Commun, 2018, 501(3):791-799
S8804 Brepocitinib (PF-06700841) Brepocitinib (PF-06700841, PF-841) 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.
S8879 Deucravacitinib (BMS-986165) Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.
S9676 Ropsacitinib (PF-06826647) Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
A5024 JAK2 Rabbit Recombinant mAb

JAK2 Rabbit Recombinant mAb detects endogenous levels of total JAK2.

A5159 JAK1 Rabbit Recombinant mAb JAK1 Rabbit Recombinant mAb detects endogenous level of JAK1.
E0011 Linderalactone Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
E0700New cucurbitacin E Cucurbitacin E (α-Elaterin; α-Elaterine), a tetracyclic triterpene derived from the climbing stem of Cucumic melo L, is an inhibitor of JAK2 and STAT3.
E0769New Ginsenoside Rh4 Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways.
E0793New G5-7 G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.
E2821New RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
S0374 GDC046 GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).
S0391 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
S0437 SAR-20347 SAR-20347 is a potent inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50 of 0.6 nM, 23 nM, 26 nM and 41 nM, respectively. SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling.
S0871 Gusacitinib (ASN-002) Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
S0981 BD750 BD750 is an immunosuppressant and a dual inhibitor of JAK3 and STAT5 that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.5 μM and 1.1 μM for mouse and human T-cell proliferation, respectively.
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, Abl1(T315I). Phase 2.
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
Sci Rep, 2022, 12(1):7
Mol Syst Biol, 2021, 17(9):e10426
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42, Zinc02557947) 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.
J Exp Med, 2022, 219(4)e20211498
Cancer Lett, 2022, 544:215812
J Headache Pain, 2022, 23(1):25
S1349 SC99 SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway by docking into the ATP-binding pocket of JAK2, also inhibits phosphorylation of JAK2and STAT3 with no effects on the other kinases associated with STAT3 signaling.
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. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Blood, 2022, blood.2021014304
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Blood, 2022, blood.2021012366
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Mol Neurodegener, 2022, 17(1):7
Int J Mol Sci, 2022, 23(8)4077
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.
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
Sci Rep, 2022, 12(1):7
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. AZ 960 induces apoptosis and growth arrest.
Cancers (Basel), 2022, 14(6)1575
BMC Cancer, 2021, 21(1):1213
Carcinogenesis, 2020, 41(7):993-1004
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Stem Cell, 2021, S1934-5909(21)00344-1
Cancer Res, 2021, canres.0955.2021
S2407 Curcumol Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities.
J Ethnopharmacol, 2021, 280:114413
Cell Prolif, 2020, 53(3):e12762
Phytother Res, 2020, 10.1002/ptr.6968
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.
Int J Mol Sci, 2022, 23(9)4597
Sci Rep, 2022, 12(1):7
Elife, 2021, 10e60646
S2692 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-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.
EBioMedicine, 2022, 78:103963
FASEB J, 2022, 36(6):e22336
Sci Rep, 2022, 12(1):7
S2736 Fedratinib (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. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
J Immunother Cancer, 2022, 10(1)e003766
Int J Mol Sci, 2022, 23(9)4597
Int J Mol Sci, 2022, 23(4)2019
S2789 Tofacitinib (CP-690550) 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. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis.
Blood, 2022, blood.2021012366
J Clin Invest, 2022, 132(11)e139298
J Immunother Cancer, 2022, 10(1)e003766
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. WP1066 induces apoptosis. Phase 1.
Cell Biosci, 2022, 12(1):43
Commun Biol, 2022, 5(1):105
Neurochem Res, 2022, 10.1007/s11064-022-03655-4
S2806 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
Int J Mol Sci, 2022, 23(9)4597
Sci Rep, 2022, 12(1):7
Nat Med, 2020, 10.1038/s41591-020-0926-0
S2851 Baricitinib (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. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
Blood, 2022, blood.2021012366
NPJ Digit Med, 2022, 5(1):83
J Immunother Cancer, 2022, 10(1)e003766
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.
Sci Rep, 2022, 12(1):7
Am J Transplant, 2021, 21(7):2360-2371
J Med Chem, 2020, 31
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.
Nat Commun, 2021, 12(1):2346
PLoS Pathog, 2021, 17(12):e1010174
Nat Med, 2020, 10.1038/s41591-020-0926-0
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S3566 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) 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 inhibits19 other tested kinases with IC50 less than 200 nM.
S5001 Tofacitinib (CP-690550) Citrate Tofacitinib citrate (CP-690550, Tasocitinib) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. Tofacitinib citrate has anti-infection activity.
Blood, 2022, blood.2021012366
J Clin Invest, 2022, 132(11)e139298
J Control Release, 2022, S0168-3659(22)00163-8
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib 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. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Cancer Cell, 2022, S1535-6108(21)00662-0
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Blood, 2022, blood.2021012366
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S5588 Creatine Creatine (Methylguanidoacetic acid) is a nitrogenous organic acid that occurs naturally in vertebrates. It facilitates the recycling of adenosine triphosphate (ATP) primarily in muscle and brain tissue.Creatine can inhibits the JAK-STAT1 signal transmission by inhibiting the interaction of IFN-γ receptors with JAK2 in an ATP-independent manner, thereby inhibiting downstream pro-inflammatory gene expression.
Cancer Cell, 2021, S1535-6108(21)00445-1
Histochem Cell Biol, 2021, 156(3):227-237
S5754 Baricitinib phosphate Baricitinib phosphate (INCB-028050, LY-3009104) 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. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19.
Arthritis Res Ther, 2022, 24(1):43
Immunol Res, 2022, 10.1007/s12026-022-09261-4
J Immunother Cancer, 2021, 9(6)e002305
S5902 1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-Hexabromocyclohexane (NSC7908) 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 JANEX-1 JANEX-1 (WHI-P131) 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).
Exp Biol Med (Maywood), 2020, 1535370220942470
S5904 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.
J Med Chem, 2020, 31
S5917 Solcitinib Solcitinib (GLPG0778, GSK2586184) 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.
Cancer Lett, 2021, 510:37-47
bioRxiv, 2021, N/A
Front Immunol, 2020, 11:1303
S6521 WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM.
S6524 NSC 42834 NSC42834 (JAK2 Inhibitor V, Z3) is an inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2 with IC50 values between 10 and 30 μM.
S6789 JAK Inhibitor I (Pyridone 6) JAK Inhibitor I (Pyridone 6, CMP 6, Compound 6) is a pan-JAK inhibitor with IC50s of 1 nM, 1 nM, 5 nM and 15 nM for JAK2, TYK2, JAK3 and JAK1, respectively.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
S7002New Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
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.
Sci Rep, 2022, 12(1):7
Molecules, 2021, 26(3)606
J Med Chem, 2020, 31
S7119 Go6976 Go6976 (PD406976) 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 Biosci, 2022, 12(1):43
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Biochimie, 2021, 184:8-17
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.
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.
NPJ Precis Oncol, 2021, 5(1):75
Oncogene, 2019, 38(9):1477-1488
J Pathol, 2019, 10.1002/path.5280
S7198 BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cell Rep, 2022, 38(12):110538
J Cell Physiol, 2022, 10.1002/jcp.30724
S7259 FLLL32 FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. FLLL32 inhibits the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
Syst Biol Reprod Med, 2022, 1-15
Pathol Oncol Res, 2022, 28:1610273
Int Immunopharmacol, 2021, 92:107304
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.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Pharmacol Res, 2022, 182:106318
Sci Rep, 2022, 12(1):7
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.
Haematologica, 2022, 10.3324/haematol.2021.279848
Sci Rep, 2022, 12(1):7
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7634 Cerdulatinib (PRT062070) hydrochloride Cerdulatinib (PRT-062070, PRT2070) hydrochloride 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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Lett, 2021, 512:28-37
S7650 Peficitinib (ASP015K) Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
S7812 Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
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.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
Int J Biol Sci, 2019, 15(9):1882-1891
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.
Clin Transl Med, 2022, 12(6):e894
J Innate Immun, 2022, 1-11
Sci Rep, 2022, 12(1):7
S8152 Cucurbitacin I

Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3.

S8162 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.
J Dermatol Sci, 2022, S0923-1811(22)00092-5
J Clin Med, 2021, 10(7)1431
Platelets, 2021, 1-12
S8195 Oclacitinib maleate Oclacitinib maleate (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.
Sci Rep, 2022, 12(1):7
Platelets, 2021, 1-12
Carcinogenesis, 2020, 41(7):993-1004
S8538 Ritlecitinib (PF-06651600) Ritlecitinib (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.
Drug Des Devel Ther, 2022, 16:363-374
Front Oncol, 2021, 11:807200
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.
Commun Biol, 2020, 3:8
S8684 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.
S8765 Abrocitinib (PF-04965842) Abrocitinib (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.
Int J Med Sci, 2020, 18;17(5):609-619
Cell Death Dis, 2019, 10(4):319
Biochem Biophys Res Commun, 2018, 501(3):791-799
S8804 Brepocitinib (PF-06700841) Brepocitinib (PF-06700841, PF-841) 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.
S8879 Deucravacitinib (BMS-986165) Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.
S9676 Ropsacitinib (PF-06826647) Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
A5024 JAK2 Rabbit Recombinant mAb

JAK2 Rabbit Recombinant mAb detects endogenous levels of total JAK2.

A5159 JAK1 Rabbit Recombinant mAb JAK1 Rabbit Recombinant mAb detects endogenous level of JAK1.
E0700New cucurbitacin E Cucurbitacin E (α-Elaterin; α-Elaterine), a tetracyclic triterpene derived from the climbing stem of Cucumic melo L, is an inhibitor of JAK2 and STAT3.
E0769New Ginsenoside Rh4 Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways.
E0793New G5-7 G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.
E2821New RGB-286638 free base RGB-286638 free base is a Cyclin-dependent kinase (CDK) inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
S7002New Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
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