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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.
- 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.
- $42.4
- $53
SizeQTY
Cited - DelgocitinibT150961263774-59-9Delgocitinib (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.
- $172
SizeQTY - Ruxolitinib phosphateT30431092939-17-7Ruxolitinib 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.
- $44
SizeQTY Cited - DeucravacitinibT146871609392-27-9Deucravacitinib (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.
- $64
SizeQTY - 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 - RitlecitinibT53821792180-81-4Ritlecitinib (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.
- $39
SizeQTY - 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 - 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 - ItacitinibT39981334298-90-6Itacitinib (INCB039110) is an orally bioavailable Janus-associated kinase 1 (JAK1) inhibitor with potential antineoplastic activity.
- $45
SizeQTY Cited - 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
- BaricitinibT24851187594-09-7Baricitinib (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.
- $43
SizeQTY Cited - 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 - 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 - 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 - 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 - OICR-9429T69161801787-56-3OICR-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.
- $31
SizeQTY Cited - (E/Z)-ZotiraciclibT21503937270-47-8(E Z)-Zotiraciclib ((E Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively.
- $38
SizeQTY - GolidocitinibT104312091134-68-6Golidocitinib (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.
- $97
SizeQTY - Prim-O-glucosylcimifuginT380580681-45-4Prim-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.
- $55
SizeQTY - 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 - LondamocitinibT117062241039-81-4Londamocitinib (JAK1-IN-7) is a selective and potent JAK1 inhibitor with anti-inflammatory activity.
- $189
SizeQTY - 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 - Jolkinolide BT2S104037905-08-1Jolkinolide 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.
- $60
SizeQTY - PonicidinT2S197552617-37-5Ponicidin (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.
- $64
SizeQTY - GDC-0214T98261831144-46-7GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
- $89
SizeQTY - DecernotinibT2636944842-54-0Decernotinib (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.
- $44
SizeQTY - PeficitinibT6933944118-01-8Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
- $38
SizeQTY Cited - KurarinoneT5S099334981-26-5Kurarinone 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.
- $39
SizeQTY - SHR0302T91951445987-21-2SHR0302 (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).
- $163
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
- TAK-659 hydrochlorideT42091952251-28-3TAK-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.
- $33
SizeQTY - TG101209T3065936091-14-4TG101209 is a selective JAK2 inhibitor with an IC50 of 6 nM.
- $40
SizeQTY - RO8191T22142691868-88-9RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.
- $38
SizeQTY Cited - LorpucitinibT620532230282-02-5Lorpucitinib (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.
- $228
SizeQTY - AbrocitinibTQ00371622902-68-4Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
- $77
SizeQTY - FilgotinibT19291206161-97-8Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 values of 10 nM for JAK1, 28 nM for JAK2, 810 nM for JAK3, and 116 nM for TYK2.
- $33
SizeQTY Cited - LinderalactoneT5S1897728-61-01. 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.
- $38
SizeQTY - Tofacitinib CitrateT2398540737-29-9Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1 2 3 (IC50s: 1 20 112 nM).
- $32
SizeQTY - IcaritinT3398118525-40-9Icaritin (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.
- $30
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 - Cucurbitacin ITQ01962222-07-3Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2 STAT3 with anti-cancer activity.
- $77
SizeQTY Cited - IlginatinibT122661239358-86-1Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor.
- $58
SizeQTY - 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 - JAK-IN-10T13571916741-98-5In houseJAK-IN-10 is a JAK inhibitor that can be used for the research of dry eye disorders.
- $79
SizeQTY - Oclacitinib maleateT69141640292-55-2Oclacitinib 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.
- $33
SizeQTY - 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 - AZ960T6309905586-69-8AZ960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 nM).
- $67
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 - JAK2 Inhibitor VT3042195371-52-9JAK2 Inhibitor V (JAK2 Inhibitor V Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.
- $33
SizeQTY
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