||Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
||Momelotinib is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP bind
||GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
||WHI-P154 is a potent JAK3 inhibitor.
||Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
||Oclacitinib(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM).
||WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.
||Janex-1 is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Syk or SRC tyrosine k
||WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3. WP1066 has been used in tria
||TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
||Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
||Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
||Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
||Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
||AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and
||Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
||LY2784544(Gandotinib) is a potent JAK2 inhibitor (IC50: 3 nM), effective in JAK2V617F(Ki: 0.245 nM). The selectivity is higher 8- and 20-fold than JAK1 and JAK3.
||TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
||Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
||JAK2 Inhibitor V
||NSC 42834(JAK2 Inhibitor V, Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.
||Ruxolitinib (INCB-18424) phosphate
||Ruxolitinib phosphate(INCB018424 phosphate) 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
||TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
||AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
||AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been used in trials stud
||XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
||GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
||Pyridone 6(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker aff
||WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
||Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL c
||Solcitinib (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.
||Mollugin may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic
||Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
||TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and
||SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
||SB1317 hydrochloride (1204918-72-8(free base))
||SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
||Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
||Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. A
||Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
||Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
||PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
||NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
||AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
||Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
||BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
||FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
||<p>Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit
||OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.
||CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
||Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.
||AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM
||WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from
||FM381 is a potent covalent reversible inhibitor of JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
||WDR5-0103 hydrochloride[890190-22-4(free base)]
||WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
||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.
||PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
||JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM
||Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
||CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell).
||PF-06700841 is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). It also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
||Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
||Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic
||ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11nM).
||Ganoderic acid B
||Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards therapeutic window of
||Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease treatment.
||MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
||MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
||PF-06700841 P-Tosylate is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).
||JAK-IN-11 is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
||AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).
||AZD4205 is a selective JAK1 inhibitor (IC50: 73 nM) and weakly inhibits JAK2/JAK3 (IC50: >14.7, >30 μM).
||BMS-986165 inhibits IL-12/23 and type I IFN pathways. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, Whic
||Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
||Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
||Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
||JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). JAK1-IN-4 is an effective and selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JA
||JAK3-IN-7 is an effective and selective JAK3 inhibitor (IC50 <0.01 μM) extracted from patent WO2011013785A1.
||ITK inhibitor 2
||ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor , with an IC50 of 2 nM.
||JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
||JAK3 covalent inhibitor-1
||JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
||JAK-IN-5 is an inhibitor of JAK.
||Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), w
||JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
||JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mutant-selective, allos
||JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
||JDTic has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to the kappa opioid recep
||BD750 is a JAK3/STAT5 inhibitor and an effective immunosuppressant that inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation with IC50 of 1.1 μM and 1.5 μM in human an
||TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR, and RET
||Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part, through downregulat
||Ponicidin has anti-leukemia, immunoregulatory and anti-inflammatory functions, it also has anti-viral function especially in the upper respiratory tract infection. Ponicidin has an
||Brevilin A is a strong impetus for the development of selective JAK-STAT inhibitors and therapeutic drugs in order to improve survival of patients with hyperactivated JAKs and STAT
||Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflamma
||Cucurbitacin E has prevention of neurodegeneration, it has potent anti-proliferative, antineoplastic, anti-inflammatory and analgesic actions, it also exhibits immunosuppressive ef
||Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IÎºB/NF-ÎºB inflammation signal path
||1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airway disease as a lead
||2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-ÎºB signaling to limit the inflammation and oxidati
||Agrimonolide is a potential α1 adrenergic receptor antagonist, it exerts anti-inflammatory activity, at least in part, via suppressing LPS-induced activation of JAK-STATs and p38
||Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway, and can be furth
||Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inh
||Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth thro