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(195)
Angiogenesis Filter
Angiogenesis Chromatin/EpigeneticAMPK
(288)
Aurora Kinase
(177)
DNA Methyltransferase
(108)
Epigenetic Reader Domain
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(72)
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(256)
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(153)
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(222)
Histone Methyltransferase
(548)
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(12)
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(475)
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(34)
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(53)
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(428)
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(363)
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(195)
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(222)
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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.
Ruxolitinib
Cited
INCB018424, (R)-Ruxolitinib
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.
- $53
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CitedOsunprotafib Cited
Osunprotafib, AC484, AC 484, ABBV-CLS-484
T616992489404-97-7In house
Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]
- $455
Size
QTY
CitedGusacitinib
ASN-002
T143311425381-60-7
Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
- $35
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Upadacitinib Cited
ABT-494
T75031310726-60-3
Upadacitinib (ABT-494) is a highly potent, selective, and orally active JAK1 inhibitor with an IC₅₀ of 43 nM; its selectivity for JAK1 is approximately 74 times that for JAK2. Upadacitinib is being investigated for the treatment of autoimmune diseases such as rheumatoid arthritis and ankylosing spondylitis.
- $53
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CitedBaricitinib Cited
LY3009104, INCB028050
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.
- $43
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CitedDeucravacitinib
BMS-986165
T146871609392-27-9
Deucravacitinib 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.
- $54
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Resveratrol Cited
trans-Resveratrol, SRT 501
T1558501-36-0
Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.
- $36
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CitedJAK-IN-11
R-348
T12549916742-11-5In house
JAK-IN-11 (R-348) is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
- $298
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Tofacitinib Cited
Tasocitinib, CP-690550
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.
- $30
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CitedRuxolitinib phosphate Cited
Ruxolitinib (INCB-18424) phosphate, INCB018424 phosphate, INCB018424, INC424, INC 424 phosphate
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.
- $44
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CitedDelgocitinib
JTE-052, Corectim(Delgocitinib)
T150961263774-59-9
Delgocitinib (JTE-052) is a JAK inhibitor and a specific JAK1/2/3/Tyk2 inhibitor (IC50=2.6-58 nM) that blocks multiple cytokine signaling pathways and inhibits pruritus, used for research on inflammatory and autoimmune diseases.
- $172
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Ritlecitinib
PF-06651600
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.
- $33
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Ponicidin
Rubescensine B
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.
- $55
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Abrocitinib
PF-04965842
TQ00371622902-68-4
Abrocitinib (PF-04965842) (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).
- $34
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Degrasyn Cited
WP1130
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).
- $35
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CitedAtractylenolide 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
- $36
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CitedKurarinone Cited
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.
- $39
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CitedPentagalloylglucose Cited
Penta-O-galloyl-β-D-glucose, 1,2,3,4,6-Penta-O-galloyl-beta-D-glucopyranose, 1,2,3,4,6-O-Pentagalloylglucose
T379414937-32-7
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a natural product functioning as an apoptosis and autophagy inducer. Possessing oral bioavailability, this compound exhibits diverse pharmacological effects including antiviral and antitumor activities through modulation of the GSK3β/β-catenin and p53 signaling pathways.
- $35
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CitedOICR-9429 Cited
OICR 9429
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.
- $31
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CitedGolidocitinib
AZD4205
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.
- $42
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JI6
JAK3 Inhibitor VI
T64370856436-16-3In house
JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.
- $163
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Fedratinib Cited
TG-101348, SAR 302503
T1995936091-26-8
Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
- $45
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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.
- $160
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Peficitinib Cited
JNJ-54781532, ASP015K
T6933944118-01-8
Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
- $34
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