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Angiogenesis Chromatin/EpigeneticAMPK
(118)
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(74)
DNA Methyltransferase
(34)
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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.
- FedratinibT1995936091-26-8Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
- $45
SizeQTY
Cited - RuxolitinibT1829941678-49-5Ruxolitinib (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.
- $53
SizeQTY Cited - KurarinoneT5S099334981-26-5Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflammatory skin diseases through the suppression of pathogenic CD4(+) T-cell differentiation and the overall immune response.
- $39
SizeQTY - RitlecitinibT53821792180-81-4Ritlecitinib (PF-06651600) is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
- $39
SizeQTY - Ruxolitinib phosphateT30431092939-17-7Ruxolitinib phosphate (INCB018424)(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 JAK3.
- $44
SizeQTY Cited - Cucurbitacin ITQ01962222-07-3Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
- $77
SizeQTY Cited - TAK-901T2709934541-31-8TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
- $66
SizeQTY Cited - JAK3iT276501918238-72-8In houseJAK3i 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.
- $350
SizeQTY
- FosifidancitinibT386241237168-58-9Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.
- $148
SizeQTY - JI069T77672850019-35-1JI069 (WAY-354189) is a potent STAT3 inhibitor that inhibits gp130 signaling by inducing dissociation between gp130 and JAK1.
- $195
SizeQTY - NVP-BSK805 2HCl (1092499-93-8(free base))T6294 In houseNVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.
- $53
SizeQTY - WDR5-0103 hydrochloride[890190-22-4(free base)]T5140WDR5-0103 hydrochloride[890190-22-4(free base)] (WD-Repeat Protein 5-0103) is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
- $37
SizeQTY - GDC-0214T98261831144-46-7GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
- $148
SizeQTY - TG-46T20743936091-15-5In houseTG-46 (TG46) inhibits JAK2, FLT3, RET, JAK3 and can be used to study glaucoma.
- $195
SizeQTY - JAK-STAT-IN-1T786071236666-76-4In houseJAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.
- $195
SizeQTY - $195
- WHI-P97 HClT4657LWHI-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 kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner.
- $58
SizeQTY - JAK-IN-10T13571916741-98-5In houseJAK-IN-10 is a JAK inhibitor. JAK-IN-10 can be used for the research of dry eye disorders.
- $79
SizeQTY - SB1317 hydrochloride (1204918-72-8(free base))T4227SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2 JAK2 FLT3 (IC50: 13 73 56 nM).
- $45
SizeQTY - ButyzamideT678941110767-45-7In houseButyzamide 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.
- $285
SizeQTY - GS-829845T679051257705-09-1In houseGS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.
- $39
SizeQTY - TG-89T20742936091-56-4In houseTG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.
- $56
SizeQTY - JAK-IN-5 hydrochlorideT11710L2751323-21-2In houseJAK-IN-5 hydrochloride is a JAK inhibitor [1].
- $1,620
SizeQTY - JAK3/BTK-IN-1T98142674036-91-8In houseJAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.
- $1,330
SizeQTY - JAK3/BTK-IN-2T98132674036-93-0In houseJAK3/ BTk-in-2 is a potent JAK3/BTK inhibitor. JAK3/ BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3/ BTk-in-2 simultaneously inhibits the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.
- $1,330
SizeQTY - IzencitinibT358982051918-33-1In houseIzencitinib (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.
- $88
SizeQTY - $88
- JAK-IN-11T12549916742-11-5In houseJAK-IN-11 (R-348) is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
- $497
SizeQTY - MomelotinibT18491056634-68-4Momelotinib (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.
- $32
SizeQTY Cited - SolcitinibT36201206163-45-2Solcitinib (GLPG-0778) (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.
- $31
SizeQTY Cited - CEP-33779T61221257704-57-6CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
- $38
SizeQTY Cited - AZD-1480T3069935666-88-9AZD1480 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 studying the treatment of Solid Malignancies, Post-Polycythaemia Vera, Primary
- $52
SizeQTY Cited - SB1317T26531204918-72-8SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).
- $64
SizeQTY Cited - Pyridone 6T3080457081-03-7Pyridone 6 (JAK Inhibitor)(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 affinities (130 nM to 10 mM) for other protein tyrosine kinases.
- $75
SizeQTY Cited - DegrasynT6300856243-80-6Degrasyn (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).
- $58
SizeQTY Cited - PacritinibT6020937272-79-2Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
- $34
SizeQTY Cited - PeficitinibT6933944118-01-8Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
- $60
SizeQTY Cited - AG490T2600133550-30-8AG490 (Tyrphostin B42) 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 Src.
- $43
SizeQTY Cited - MubritinibT6124366017-09-6Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2 ErbB2 with IC50 of 6 nM.
- $32
SizeQTY Cited - TofacitinibT6321477600-75-2Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
- $30
SizeQTY Cited - BaricitinibT24851187594-09-7Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
- $43
SizeQTY Cited - AT9283T3068896466-04-9AT9283 (J-504568) 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).
- $39
SizeQTY Cited - Atractylenolide IT5S016773069-13-31. 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
- $36
SizeQTY Cited - WP1066T2156857064-38-1WP1066 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.
- $44
SizeQTY Cited - UpadacitinibT75031310726-60-3Upadacitinib (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.
- $39
SizeQTY Cited - FilgotinibT19291206161-97-8Filgotinib (GLPG0634) 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.
- $50
SizeQTY Cited - PP2T6266172889-27-9PP2 (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.
- $39
SizeQTY Cited - RO8191T22142691868-88-9RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.
- $38
SizeQTY Cited - LFM-A13T6217244240-24-2LFM-A13（IC50=2.5 μM）, a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.
- $31
SizeQTY Cited - CurcumolT28534871-97-0Curcumol ((-)-Curcumol), a pure monomer isolated extracted from Rhizoma Curcumaeis, has antitumor activities.
- $43
SizeQTY Cited - AZ960T6309905586-69-8AZ960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
- $67
SizeQTY Cited
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