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. |
Selective |
|
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. |
Selective |
|
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.
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Selective |
|
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. |
Selective |
|
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. |
Selective |
|
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. |
Selective |
|
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. |
Selective |
|
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. |
Selective |
JAK2, IC50: 0.26 nM |
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. |
Selective |
JAK2, IC50: <3 nM; JAK2, Ki: 0.45 nM |
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. |
Selective |
JAK2, IC50: ~0.5 nM |
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. |
Selective |
JAK2, IC50: 1.1 nM |
S2806 |
CEP-33779 |
CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2. |
Selective |
JAK2, IC50: 1.8 nM |
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. |
Selective |
JAK2, IC50: 2.2 nM |
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. |
Selective |
JAK2, IC50: 3 nM; JAK2 (V617F), IC50: 3 nM |
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. |
Selective |
JAK2, IC50: 6 nM |
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. |
Selective |
JAK2, IC50: 19 nM |
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. |
Selective |
JAK2, IC50: 2.3 μM |
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.
|
Selective |
JAK2, IC50: <5 μM |
S0391 |
TG-89 |
TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. |
Selective |
JAK2, IC50: 11.2 μM |
S2407 |
Curcumol |
Curcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities. |
Selective |
|
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. |
Selective |
|
S7650 |
Peficitinib |
Peficitinib is an orally bioavailable JAK inhibitor. Phase 3.
|
Selective |
|
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. |
Selective |
|
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. |
Selective |
|
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. |
Selective |
|
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.
|
Selective |
|
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.
|
Selective |
|
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. |
Pan |
JAK2, IC50: 3 nM; JAK2, Ki: 0.288 nM; JAK2 (V617F), Ki: 0.245 nM |
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. |
Pan |
JAK2, IC50: 1 nM |
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). |
Pan |
JAK2, IC50: 1.2 nM |
S8802 |
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. |
Pan |
JAK2, IC50: 2.6 nM |
S1378 |
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. |
Pan |
JAK2, IC50: 2.8 nM |
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. |
Pan |
JAK2, IC50: 2.8 nM |
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. |
Pan |
JAK2, IC50: 2.8 nM |
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. |
Pan |
JAK2, IC50: 5.7 nM |
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. |
Pan |
JAK2, IC50: 5.7 nM |
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. |
Pan |
JAK2, IC50: 6 nM |
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.
|
Pan |
JAK2, IC50: 6 nM |
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.
|
Pan |
JAK2, Ki: 13 nM |
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. |
Pan |
JAK2, IC50: 18 nM |
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. |
Pan |
JAK2, IC50: 18nM |
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. |
Pan |
JAK2, IC50: 23 nM; JAK2 (V617F), IC50: 19 nM |
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. |
Pan |
JAK2, IC50: 20 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. |
Pan |
JAK2, IC50: 20 nM |
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. |
Pan |
JAK2, IC50: 26 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. |
Pan |
JAK2, Ki: 27.6 nM |
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.
|
Pan |
JAK2, IC50: 28 nM |
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). |
Pan |
JAK2, IC50: 74 nM |
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. |
Pan |
JAK2, IC50: 77 nM |
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. |
Pan |
JAK2, IC50: 109 nM |
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. |
Pan |
JAK2, Ki: 740 nM |
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. |
Pan |
JAK2, IC50: 803 nM |
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. |
Pan |
|