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JAK
T10009 JAK3-IN-7 JAK3-IN-7 is an effective and selective JAK3 inhibitor (IC50 <0.01 μM) extracted from patent WO2011013785A1.
T10424 AZ-3 AZ-3 is a potent and selective JAK1 inhibitor (IC50: 34 nM).
T10431 AZD4205 AZD4205 is a selective JAK1 inhibitor (IC50: 73 nM) and weakly inhibits JAK2/JAK3 (IC50: >14.7, >30 μM).
T11690 ITK inhibitor 2 ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor , with an IC50 of 2 nM.
T11708 JAK2-IN-4 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.
T11709 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.
T11710 JAK-IN-5 JAK-IN-5 is an inhibitor of JAK.
T11711 Jaspamycin 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
T11713 JBJ-02-112-05 JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
T11714 JBJ-04-125-02 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
T11721 JDTic 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
T11721L JDTic dihydrochloride JDTic is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
T12091 MM-589 MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12091L MM-589 TFA MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.
T12427 PF-06700841 (P-Tosylate) PF-06700841 P-Tosylate is a potent dual inhibitor of Janus kinase 1 (JAK1) and TYK2 (IC50s of 17 nM and 23 nM, respectively).
T12549 JAK-IN-11 JAK-IN-11 is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
T14331 Gusacitinib Gusacitinib (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
T14687 BMS-986165 BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases
T15037 Momelotinib Mesylate Momelotinib Mesylate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T15038 Momelotinib sulfate Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
T15096 Delgocitinib Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
T15606 JAK1-IN-4 JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (I
T16995 TAS05567 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
T17019 TCS 21311 TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >10
T1829 Ruxolitinib 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).
T1849 Momelotinib 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
T1929 Filgotinib 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.
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T1995 Fedratinib Fedratinib (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
T2012 Oclacitinib 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).
T2035 WHI-P258 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.
T2045 WHI-P131 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 ki
T2156 WP1066 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
T2341 KW2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.
T2360 Baricitinib Phosphate Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2398 Tofacitinib Citrate Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
T2460 JAK 3 inhibitor IV JAK 3 inhibitor IV is a 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.
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
T2487 Cerdulatinib Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
T2600 AG490 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
T2636 Decernotinib 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.
T2638 Gandotinib 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.
T2709 TAK901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
T2853 Curcumol Curcumol, a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
T2S1040 Jolkinolide B 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
T2S1975 Ponicidin 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
T3024 Avitinib Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic
T3042 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.
T3043 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
T3065 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
T3068 AT9283 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).
T3069 AZD1480 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
T3072 XL019 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1.
T3076 GLPG0634 analogue GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
T3080 Pyridone 6 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
T3201 WDR5-0103 WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T3398 Icaritin Icaritin has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL c
T3620 Solcitinib Solcitinib (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.
T3673 Mollugin 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
T3998 Itacitinib Itacitinib is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.
T4209 TAK-659 hydrochloride 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
T4210 SAR20347 SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
T4227 SB1317 hydrochloride (1204918-72-8(free base)) SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
T4657 WHI-P97 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
T4657L WHI-P97 HCl 211555-05-4(free base) WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinas
T4657L WHI-P97 HCl 211555-05-4(free base) WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinas
T4672 Brevilin A Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor activity. Brevilin
T5049 NVP-BSK805 NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
T5091 FM381 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.
T5140 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).
T5382 PF-06651600 PF-06651600 is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
T5492 JAK3-IN-6 JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM
T5S0993 Kurarinone Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect o
T6020 Pacritinib Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
T6104 Cerdulatinib hydrochloride 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
T6122 CEP33779 CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
T6124 Mubritinib Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
T6145 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.
T6156 S-Ruxolitinib Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
T6266 PP2 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.
T6309 AZ 960 AZ 960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T6790 BMS911543 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.
T6838 FLLL32 FLLL32 is an effective JAK2/STAT3 inhibitor (IC50 of <5 μM).
T6914 Oclacitinib maleate 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 a
T6916 OICR9429 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.
T6920 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
T7503 Upadacitinib 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.
T8546 BD750 BD750 is an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation(IC50 of 1.5 μM and 1.1 μM in mouse and human T
T8719 SC99 SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation and displays pote
T8742 JAK2 inhibitor G5-7 JAK2 inhibitor G5-7 is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 h
TJS1779 Protosappanin A Protosappanin A has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal path
TMA1743 Ergosterol peroxide Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inh
TN1059 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
TN2002 Obovatol Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease treatment.
TN2511 1,6-O,O-Diacetylbritannilactone 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
TN2775 2-Methoxystypandrone 2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidati
TN3364 Agrimonolide 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
TN3541 Broussonin E 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
TN4774 Physalin A 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
TQ0010 PF-06700841 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).
TQ0037 Abrocitinib Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
TQ0061 CHZ868 CHZ868 is a type II JAK2 inhibitor (IC50: 0.17 μM in EPOR JAK2 WT Ba/F3 cell).
TQ0196 Cucurbitacin I Cucurbitacin I, a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
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