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Angiogenesis Filter
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JAK
The JAK-STAT signalling pathway is a chain of interactions between proteins in a cell, and is involved in processes such as immunity, cell division, cell death and tumour formation. There are 4 JAK proteins: JAK1, JAK2, JAK3 and TYK2. JAKs contains a FERM domain (approximately 400 residues), an SH2-related domain (approximately 100 residues), a kinase domain (approximately 250 residues) and a pseudokinase domain (approximately 300 residues). The kinase domain is vital for JAK activity, since it allows JAKs to phosphorylate (add phosphate groups to) proteins.
FilterHomeSignaling PathwaysStem Cells-Angiogenesis-Tyrosine Kinase/Adaptors-Chromatin/Epigenetic-JAK/STAT signalingJAK
Ruxolitinib
Cited
T1829941678-49-5
Ruxolitinib (INCB018424) is a JAK1 2 inhibitor (IC50=3.3 2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
- 50 €
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CitedDelgocitinib
T150961263774-59-9
Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.
- 163 €
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Ruxolitinib phosphate Cited
T30431092939-17-7
Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1 2 inhibitor with IC50 of 3.3 nM 2.8 nM. Its selectivity for JAK1 2 is more than 130 times that of JAK3.
- 41 €
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CitedDeucravacitinib
T146871609392-27-9
Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12 23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.
- 60 €
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Upadacitinib Cited
T75031310726-60-3
Upadacitinib (ABT-494) (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.
- 37 €
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CitedFedratinib Cited
T1995936091-26-8
Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
- 42 €
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CitedRitlecitinib
T53821792180-81-4
Ritlecitinib (PF-06651600) is an orally available, selective JAK3 inhibitor with an IC50 of 33.1 nM and does not affect the activity of JAK1 2.
- 37 €
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Baricitinib Cited
T24851187594-09-7
Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9 5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.
- 40 €
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CitedButyzamide
T678941110767-45-7In house
Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.
- 270 €
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Itacitinib Cited
T39981334298-90-6
Itacitinib (INCB039110) is an orally bioavailable Janus-associated kinase 1 (JAK1) inhibitor with potential antineoplastic activity.
- 42 €
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CitedOICR-9429 Cited
T69161801787-56-3
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.
- 29 €
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CitedTofacitinib Cited
T6321477600-75-2
Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3 2 1 (IC50=1 20 112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.
- 28 €
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CitedDegrasyn Cited
T6300856243-80-6
Degrasyn (WP1130) (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
- 55 €
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CitedWP1066 Cited
T2156857064-38-1
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 trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.
- 41 €
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Cited(E/Z)-Zotiraciclib
T21503937270-47-8
(E Z)-Zotiraciclib ((E Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively.
- 36 €
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Izencitinib
T358982051918-33-1In house
Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.
- 76 €
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Prim-O-glucosylcimifugin
T380580681-45-4
Prim-O-glucosylcimifugin (Cimifugin 7-glucoside) can inhibit the proliferation of SMC(smooth muscle cell) stimulated by TNF-alpha, increase the proportion of G0 G1 phase.
- 52 €
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Decernotinib
T2636944842-54-0
Decernotinib (VRT-831509)(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.
- 41 €
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Golidocitinib
T104312091134-68-6
Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.
- 92 €
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GDC-0214
T98261831144-46-7
GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
- 84 €
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Ponicidin
T2S197552617-37-5
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens that exhibits immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer activity. Ponicidin induces apoptosis of gastric carcinoma cells, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on the protein levels of JAK2 and STAT3.
- 60 €
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Londamocitinib
T117062241039-81-4
Londamocitinib (JAK1-IN-7) is a selective and potent JAK1 inhibitor with anti-inflammatory activity.
- 179 €
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Atractylenolide I Cited
T5S016773069-13-3
1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res
- 34 €
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CitedPacritinib Cited
T6020937272-79-2
Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23 22 nM, in cell-free assays).
- 32 €
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CitedJolkinolide B
T2S104037905-08-1
Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.
- 57 €
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PP2 Cited
T6266172889-27-9
PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck Fyn (IC50:4 5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
- 37 €
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CitedSHR0302
T91951445987-21-2
SHR0302 (ARQ252) is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times for Tyk2).
- 154 €
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JAK-STAT-IN-1
T786071236666-76-4In house
JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.
- 185 €
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TAK-659 hydrochloride
T42091952251-28-3
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 FLT3.
- 31 €
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Kurarinone
T5S099334981-26-5
Kurarinone is a flavonoid extracted from the shrub Sophora flavescens, which has anti-tumor, estrogenic and anti-inflammatory activities, and also has a strong inhibitory effect on immune responses.
- 37 €
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Peficitinib Cited
T6933944118-01-8
Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
- 32 €
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CitedLorpucitinib
T620532230282-02-5
Lorpucitinib (JNJ-64251330) is an orally available, selective and potent JAK kinase inhibitor for the study of inflammatory and gastrointestinal disorders associated with Janus kinase (JAK) signaling.
- 216 €
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Tofacitinib Citrate
T2398540737-29-9
Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1 2 3 (IC50s: 1 20 112 nM).
- 30 €
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Cucurbitacin I Cited
TQ01962222-07-3
Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2 STAT3 with anti-cancer activity.
- 73 €
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CitedAbrocitinib
TQ00371622902-68-4
Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29 803 nM for JAK1 2).
- 73 €
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Linderalactone
T5S1897728-61-0
1. Linderalactone showed significant inhibitory effects on superoxide anion generation by human neutrophils in response to fMLP CB, values of IC5 is 8.48 μg mL.
- 36 €
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Icaritin Cited
T3398118525-40-9
Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6 JAK2 STAT3 signaling. Icaritin at low concentration (4 or 8 μMol L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.
- 28 €
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CitedIlginatinib
T122661239358-86-1
Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor.
- 55 €
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CHZ868
TQ00611895895-38-1
CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.
- 63 €
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JAK-IN-10
T13571916741-98-5In house
JAK-IN-10 is a JAK inhibitor that can be used for the research of dry eye disorders.
- 75 €
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Oclacitinib maleate
T69141640292-55-2
Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members, with IC50 values ranging from 10 to 99 nM, and JAK1-dependent cytokines, with IC50 ranging from 36 to 249 nM, while not inhibiting a panel of 38 non-JAK kinases.
- 31 €
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AZ960 Cited
T6309905586-69-8
AZ960 is an effective ATP competitive JAK2 inhibitor (IC50 Ki: <3 nM and0.45 nM).
- 63 €
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CitedFedratinib hydrochloride hydrate
T92511374744-69-0
Fedratinib hydrochloride hydrate (SAR 302503 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor.
- 37 €
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JAK3i
T276501918238-72-8In house
JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.
- 332 €
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Brevilin A
T467216503-32-5
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 A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 μM) in Cancer Cells.Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K AKT mTOR inactivation in colon adenocarcinoma cell CT26.antitumour
- 92 €
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Momelotinib Cited
T18491056634-68-4
Momelotinib (LM-1149) 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 binding, which may result in inhibition of JAK1 2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1 2-expressing tumor cells.
- 30 €
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CitedRO8191 Cited
T22142691868-88-9
RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.
- 36 €
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