JAK

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JAK製品

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S1378 Ruxolitinib ルクソリチニブ (Ruxolitinib (INCB018424)) は、最初に臨床試験が行われた強力で選択的なJAK1/2 阻害剤であり、IC50 はそれぞれ 3.3 nM/ 2.8 nM、JAK1/2 に対して JAK3 の 130 倍の選択性を示します。ルクソリチニブはマイトファジー (mitophagy) によって抗腫瘍作用を示します。また、オートファジー (autophagy) を誘導し、アポトーシス (apoptosis) を促進します。
Acta Neuropathol, 2024, 147(1):28
Theranostics, 2024, 14(3):1224-1240
Cell Rep, 2024, 43(2):113600.
S5001 Tofacitinib (CP-690550) Citrate トファシチニブクエン酸塩 (Tofacitinib citrate (CP-690550、タソシチニブ)) は JAK の新規阻害剤です。IC50は JAK3, JAK2, JAK1 に対してそれぞれ 1 nM, 20 nM, 112 nM です。 トファシチニブクエン酸塩は抗感染作用を持ちます。
Inflamm Regen, 2023, 43(1):44
Front Immunol, 2023, 14:1097383
Front Immunol, 2023, 14:1097383
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.
Virol J, 2024, 21(1):23
Int J Mol Sci, 2023, 24(7)6228
Front Oncol, 2023, 13:1043694
S2789 Tofacitinib Tofacitinib 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.
Cell Rep Med, 2024, S2666-3791(23)00615-8
Dis Model Mech, 2024, 17(1)dmm050541
Nature, 2023, 615(7951):305-314
S1143 AG-490 AG-490 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.
Cytotherapy, 2024, 26(2):145-156
J Neuroinflammation, 2023, 20(1):87
iScience, 2023, 26(11):108211
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.
Sci Rep, 2024, 14(1):4125
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Cancer Res, 2023, 83(2):264-284
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.
Cell Rep, 2024, 43(2):113751
PLoS One, 2024, 19(1):e0295629
Adv Sci (Weinh), 2023, 10(24):e2302613
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.
Cancer Cell Int, 2024, 24(1):60
Cancer Immunol Res, 2023, 11(3):290-305
Cancer Immunol Res, 2023, 11(3):290-305
S2851 Baricitinib Baricitinib 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.
Sci Rep, 2024, 14(1):4125
Nat Cancer, 2023, 4(7):984-1000
Nat Cancer, 2023, 4(7):984-1000
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.
Cell Rep, 2023, 42(9):113067
Breast Cancer Res, 2023, 25(1):51
Adv Skin Wound Care, 2023, 36(5):249-258
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.
Inflamm Regen, 2023, 43(1):44
Front Immunol, 2023, 14:1087986
Burns Trauma, 2023, 11:tkad006
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.
J Cell Sci, 2023, 136(4)jcs259788
Sci Adv, 2023, 9(34):eadi5168
Sci Adv, 2023, 9(34):eadi5168
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.
Adv Sci (Weinh), 2023, 10(12):e2206542
Bone Res, 2023, 11(1):18
J Transl Med, 2023, 21(1):530
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).
PeerJ, 2023, 11:e16581
bioRxiv, 2023, 10.1101/2023.12.19.572304
Cancers (Basel), 2022, 14(21)5215
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.
Front Immunol, 2023, 14:1185570
Int Immunopharmacol, 2023, 118:109993
Int Immunopharmacol, 2023, 118:109993
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
Front Immunol, 2022, 13:1001068
Sci Rep, 2022, 12(1):7
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.
Phytomedicine, 2023, 117:154918
EBioMedicine, 2022, 78:103963
Front Immunol, 2022, 13:1001068
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.
Int J Mol Sci, 2023, 24(17)13623
Cells, 2023, 12(3)453
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Physiol Rep, 2023, 11(19):e15829
Physiol Rep, 2023, 11(19):e15829
Inflamm Regen, 2023, 43(1):44
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
Am J Transplant, 2021, 21(7):2360-2371
S8057 Pacritinib Pacritinib 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.
Sci Rep, 2024, 14(1):4125
Clin Transl Med, 2022, 12(6):e894
Front Immunol, 2022, 13:1001068
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.
Nat Commun, 2023, 14(1):6908
Nat Commun, 2023, 14(1):6908
Int J Mol Sci, 2023, 10.3390/ijms241813863
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.
Cancer Commun -Lond), 2023, 43(10):1117-1142
Microbiol Res, 2023, 276:127480
Pathol Oncol Res, 2022, 28:1610273
S2806 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
J Transl Med, 2023, 21(1):426
Int J Mol Sci, 2022, 23(9)4597
Sci Rep, 2022, 12(1):7
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.
Br J Cancer, 2023, 10.1038/s41416-023-02196-z
Cells, 2023, 12(5)770
J Exp Med, 2022, 219(11)e20212228
S8162 Upadacitinib Upadacitinib 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.
Nat Commun, 2024, 15(1):1718
Cell Mol Immunol, 2023, 10.1038/s41423-023-01012-1
Inflamm Regen, 2023, 43(1):44
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.
Front Immunol, 2022, 13:1001068
Cancers (Basel), 2022, 14(6)1575
BMC Cancer, 2021, 21(1):1213
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
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.
Int J Mol Sci, 2023, 24(17)13623
Cells, 2023, 12(9)1295
Cells, 2023, 12(9)1295
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.
Biochem Pharmacol, 2023, 215:115704
Sci Rep, 2022, 12(1):7
Molecules, 2021, 26(3)606
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.
Mol Metab, 2023, 10.1016/j.molmet.2023.101836
NPJ Precis Oncol, 2021, 5(1):75
Oncogene, 2019, 38(9):1477-1488
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
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 Res, 2023, 83(2):264-284
Pharm Biol, 2022, 60(1):899-908
Cancer Lett, 2021, 510:37-47
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
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.
Mol Metab, 2023, 10.1016/j.molmet.2023.101836
Nat Commun, 2022, 13(1):6226
Nat Commun, 2022, 13(1):6226
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.
Cells, 2022, 11(22)3588
Int J Med Sci, 2020, 18;17(5):609-619
Cell Death Dis, 2019, 10(4):319
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.
Aging (Albany NY), 2022, 14(16):6796-6808
Cancer Cell, 2021, S1535-6108(21)00445-1
Histochem Cell Biol, 2021, 156(3):227-237
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
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.
Nat Commun, 2024, 15(1):1718
Nat Commun, 2024, 15(1):1337
Front Immunol, 2023, 10.3389/fimmu.2023.1263926
S7812 Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
J Physiol, 2023, 10.1113/JP284393
Nat Chem Biol, 2022, 10.1038/s41589-022-01098-0
S7650 Peficitinib Peficitinibは生物活性を持っている一種の経口(実験動物だけにとって)JAK阻害剤です。臨床3期。
Int Immunopharmacol, 2023, 122:110630
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.
Bioengineered, 2022, 13(6):14616-14631
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
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
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
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
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.
Cancer Immunol Res, 2021, 9-5:542-553
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
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.
Cancer Discov, 2023, 13(2):410-431
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.
Cancer Sci, 2023, 114(6):2622-2633
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.
S6521 WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM.
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.
S7002 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.
E1526New Zasocitinib Zasocitinib( NDI-034858, TAK-279) is a TYK2 inhibitor, which is currently being investigated in a phase IIb trial for moderate-to-severe plaque psoriasis.
S3267 Nicotiflorin (Kaempferol-3-O-rutinoside) Nicotiflorin (Kaempferol-3-O-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.
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.
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.
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.
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.
E2821 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.
E0793 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.
E0769 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.
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.
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.
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of TYK2 with IC50 of 1.5nM on TYK2 as tested in cell-based pharmacological assays
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.
S0391 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
S8802New Delgocitinib (JTE-052) Delgocitinib (JTE-052) is a specific  JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
E0700 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.
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).
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.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
S1378 Ruxolitinib ルクソリチニブ (Ruxolitinib (INCB018424)) は、最初に臨床試験が行われた強力で選択的なJAK1/2 阻害剤であり、IC50 はそれぞれ 3.3 nM/ 2.8 nM、JAK1/2 に対して JAK3 の 130 倍の選択性を示します。ルクソリチニブはマイトファジー (mitophagy) によって抗腫瘍作用を示します。また、オートファジー (autophagy) を誘導し、アポトーシス (apoptosis) を促進します。
Acta Neuropathol, 2024, 147(1):28
Theranostics, 2024, 14(3):1224-1240
Cell Rep, 2024, 43(2):113600.
S5001 Tofacitinib (CP-690550) Citrate トファシチニブクエン酸塩 (Tofacitinib citrate (CP-690550、タソシチニブ)) は JAK の新規阻害剤です。IC50は JAK3, JAK2, JAK1 に対してそれぞれ 1 nM, 20 nM, 112 nM です。 トファシチニブクエン酸塩は抗感染作用を持ちます。
Inflamm Regen, 2023, 43(1):44
Front Immunol, 2023, 14:1097383
Front Immunol, 2023, 14:1097383
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.
Virol J, 2024, 21(1):23
Int J Mol Sci, 2023, 24(7)6228
Front Oncol, 2023, 13:1043694
S2789 Tofacitinib Tofacitinib 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.
Cell Rep Med, 2024, S2666-3791(23)00615-8
Dis Model Mech, 2024, 17(1)dmm050541
Nature, 2023, 615(7951):305-314
S1143 AG-490 AG-490 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.
Cytotherapy, 2024, 26(2):145-156
J Neuroinflammation, 2023, 20(1):87
iScience, 2023, 26(11):108211
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.
Sci Rep, 2024, 14(1):4125
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Cancer Res, 2023, 83(2):264-284
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.
Cell Rep, 2024, 43(2):113751
PLoS One, 2024, 19(1):e0295629
Adv Sci (Weinh), 2023, 10(24):e2302613
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.
Cancer Cell Int, 2024, 24(1):60
Cancer Immunol Res, 2023, 11(3):290-305
Cancer Immunol Res, 2023, 11(3):290-305
S2851 Baricitinib Baricitinib 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.
Sci Rep, 2024, 14(1):4125
Nat Cancer, 2023, 4(7):984-1000
Nat Cancer, 2023, 4(7):984-1000
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.
Cell Rep, 2023, 42(9):113067
Breast Cancer Res, 2023, 25(1):51
Adv Skin Wound Care, 2023, 36(5):249-258
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.
Inflamm Regen, 2023, 43(1):44
Front Immunol, 2023, 14:1087986
Burns Trauma, 2023, 11:tkad006
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.
J Cell Sci, 2023, 136(4)jcs259788
Sci Adv, 2023, 9(34):eadi5168
Sci Adv, 2023, 9(34):eadi5168
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.
Adv Sci (Weinh), 2023, 10(12):e2206542
Bone Res, 2023, 11(1):18
J Transl Med, 2023, 21(1):530
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).
PeerJ, 2023, 11:e16581
bioRxiv, 2023, 10.1101/2023.12.19.572304
Cancers (Basel), 2022, 14(21)5215
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.
Front Immunol, 2023, 14:1185570
Int Immunopharmacol, 2023, 118:109993
Int Immunopharmacol, 2023, 118:109993
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
Front Immunol, 2022, 13:1001068
Sci Rep, 2022, 12(1):7
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.
Phytomedicine, 2023, 117:154918
EBioMedicine, 2022, 78:103963
Front Immunol, 2022, 13:1001068
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.
Int J Mol Sci, 2023, 24(17)13623
Cells, 2023, 12(3)453
Cancer Cell, 2022, S1535-6108(22)00312-9
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.
Physiol Rep, 2023, 11(19):e15829
Physiol Rep, 2023, 11(19):e15829
Inflamm Regen, 2023, 43(1):44
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
Am J Transplant, 2021, 21(7):2360-2371
S8057 Pacritinib Pacritinib 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.
Sci Rep, 2024, 14(1):4125
Clin Transl Med, 2022, 12(6):e894
Front Immunol, 2022, 13:1001068
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.
Nat Commun, 2023, 14(1):6908
Nat Commun, 2023, 14(1):6908
Int J Mol Sci, 2023, 10.3390/ijms241813863
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.
Cancer Commun -Lond), 2023, 43(10):1117-1142
Microbiol Res, 2023, 276:127480
Pathol Oncol Res, 2022, 28:1610273
S2806 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
J Transl Med, 2023, 21(1):426
Int J Mol Sci, 2022, 23(9)4597
Sci Rep, 2022, 12(1):7
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.
Br J Cancer, 2023, 10.1038/s41416-023-02196-z
Cells, 2023, 12(5)770
J Exp Med, 2022, 219(11)e20212228
S8162 Upadacitinib Upadacitinib 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.
Nat Commun, 2024, 15(1):1718
Cell Mol Immunol, 2023, 10.1038/s41423-023-01012-1
Inflamm Regen, 2023, 43(1):44
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.
Front Immunol, 2022, 13:1001068
Cancers (Basel), 2022, 14(6)1575
BMC Cancer, 2021, 21(1):1213
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
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.
Int J Mol Sci, 2023, 24(17)13623
Cells, 2023, 12(9)1295
Cells, 2023, 12(9)1295
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.
Biochem Pharmacol, 2023, 215:115704
Sci Rep, 2022, 12(1):7
Molecules, 2021, 26(3)606
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.
Mol Metab, 2023, 10.1016/j.molmet.2023.101836
NPJ Precis Oncol, 2021, 5(1):75
Oncogene, 2019, 38(9):1477-1488
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
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 Res, 2023, 83(2):264-284
Pharm Biol, 2022, 60(1):899-908
Cancer Lett, 2021, 510:37-47
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
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.
Mol Metab, 2023, 10.1016/j.molmet.2023.101836
Nat Commun, 2022, 13(1):6226
Nat Commun, 2022, 13(1):6226
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.
Cells, 2022, 11(22)3588
Int J Med Sci, 2020, 18;17(5):609-619
Cell Death Dis, 2019, 10(4):319
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.
Aging (Albany NY), 2022, 14(16):6796-6808
Cancer Cell, 2021, S1535-6108(21)00445-1
Histochem Cell Biol, 2021, 156(3):227-237
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
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.
Nat Commun, 2024, 15(1):1718
Nat Commun, 2024, 15(1):1337
Front Immunol, 2023, 10.3389/fimmu.2023.1263926
S7812 Itacitinib (INCB39110) Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
J Physiol, 2023, 10.1113/JP284393
Nat Chem Biol, 2022, 10.1038/s41589-022-01098-0
S7650 Peficitinib Peficitinibは生物活性を持っている一種の経口(実験動物だけにとって)JAK阻害剤です。臨床3期。
Int Immunopharmacol, 2023, 122:110630
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.
Bioengineered, 2022, 13(6):14616-14631
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
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
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
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
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.
Cancer Immunol Res, 2021, 9-5:542-553
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
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.
Cancer Discov, 2023, 13(2):410-431
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.
Cancer Sci, 2023, 114(6):2622-2633
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.
S6521 WHI-P258 WHI-P258 is an inhibitor of JAK3 with Ki value of 72 μM.
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.
S7002 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.
E1526New Zasocitinib Zasocitinib( NDI-034858, TAK-279) is a TYK2 inhibitor, which is currently being investigated in a phase IIb trial for moderate-to-severe plaque psoriasis.
S3267 Nicotiflorin (Kaempferol-3-O-rutinoside) Nicotiflorin (Kaempferol-3-O-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.
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.
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.
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.
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.
E2821 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.
E0793 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.
E0769 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.
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.
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.
S0384 RO495 RO495 (CS-2667) is a potent inhibitor of TYK2 with IC50 of 1.5nM on TYK2 as tested in cell-based pharmacological assays
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.
S0391 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
S8802New Delgocitinib (JTE-052) Delgocitinib (JTE-052) is a specific  JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
E0700 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.
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).
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.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
E1526New Zasocitinib Zasocitinib( NDI-034858, TAK-279) is a TYK2 inhibitor, which is currently being investigated in a phase IIb trial for moderate-to-severe plaque psoriasis.
S8802New Delgocitinib (JTE-052) Delgocitinib (JTE-052) is a specific  JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).

JAK阻害剤の選択性比較

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