Search Result
Results for "
A jak Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
18
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-153568
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JAK
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Cancer
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JAK1-IN-11 (compound 11) is a potent inhibitor of JAK,with IC50s of 0.02 nM (JAK1),and 0.44 nM (JAK2),respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2 .
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- HY-15480
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jak2 Inhibitor V; Z3
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JAK
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Cancer
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NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
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- HY-116505
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JAK
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Cancer
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JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 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 (IC50, 227 nM) .
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- HY-155746
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JAK
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Infection
Inflammation/Immunology
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JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs) .
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- HY-161139
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JAK
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Inflammation/Immunology
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JAK1-IN-14 (Compound 12a) is a potent and selective JAK1 inhibitor. JAK1-IN-14 inhibits JAK1 and JAK2 with an IC50 value of 12.6 nM and 135 nM. JAK1-IN-14 suppresses hepatic fibrosis levels and can be used for the research of liver fibrosis and inflammatory diseases .
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- HY-100759
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JAK
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Cancer
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JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively .
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- HY-156535
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JAK
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Inflammation/Immunology
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JAK kinase-IN-1 (Example 1) is a JAK inhibitor. JAK kinase-IN-1 inhibits TYK2, JAK1, JAK2 and JAK3 with IC50 values of 4.2 nM, 32 nM, 27 nM, 3473 nM respectively .
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- HY-151285
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Apoptosis
JAK
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Inflammation/Immunology
Cancer
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JAK-2-/3-IN-3 (compound ST4j) is a potent JAK2/3 inhibitor with IC50s of 13.00 and 14.86 nM for JAK2 and JAK3, respectively. JAK-2-/3-IN-3 inhibits autophosphorylation of JAK2 and induces apoptosis in a dose- and time-dependent manner. JAK-2-/3-IN-3 can be used in studies of lymph derived diseases and leukemia .
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- HY-170439
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JAK
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Cancer
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JAK3-IN-16 (compound 6) is a covalent JAK3 inhibitor .
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- HY-147975
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JAK
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Inflammation/Immunology
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JAK3-IN-12 (compound 5k) is a highly potent JAK3 inhibitor with IC50 values of 9.5 nM, 18 nM and 42 nM for JAK3, JAK1 and JAK2, respectively. JAK3-IN-12 can be used for researching rheumatoid arthritis .
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- HY-144440
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JAK
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Cancer
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JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC50 of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more .
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- HY-137756
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JAK
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Cancer
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JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells .
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- HY-10652
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JAK
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Inflammation/Immunology
Cancer
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JAK-2/3-IN-1 is a potent JAK-2 and JAK-3 inhibitor extracted from patent US8163732B2, compound 46, has Kis of <250 nM for both isoforms .
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- HY-168059
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JAK
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Inflammation/Immunology
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JAK3-IN-15 (compound 22) is a JAK3 inhibitor that reduces LPS-induced p-JAK3 secretion. JAK3-IN-15 can be used in the study of rheumatoid arthritis .
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- HY-111750
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JAK
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Inflammation/Immunology
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JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively .
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- HY-146727
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JAK
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Inflammation/Immunology
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JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases .
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- HY-19544
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JAK
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Cancer
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JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM) .
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- HY-13827
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JAK
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Inflammation/Immunology
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JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
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- HY-133747
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JAK
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Inflammation/Immunology
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JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research .
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- HY-13961
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JAK
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Cancer
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GLPG0634 analog (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3 .
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- HY-10963
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CYT387 mesylate
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JAK
Autophagy
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Cancer
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Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
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- HY-153440
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JAK
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Cancer
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JAK-IN-25 (compound 19) is a potent JAK inhibitor with IC50s of 6 nM, 21 nM, 8 nM, 1051 nM for TYK2, JAK1, JAK2, JAK3, respectively. JAK-IN-25 inhibits human whole blood IL-12 (HEB IL-12) with an IC50 of 28 nM. JAK-IN-25 has the potential for cancer research .
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- HY-170723
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JAK
TNF Receptor
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Infection
Inflammation/Immunology
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JAK-IN-39 (compound 11) is a JAK inhibitor that suppresses JAK1, JAK2, JAK3 with IC50 values of 0.05, 1.18, and 0.03 nM, respectively. JAK-IN-39 can inhibit the viability of TF-1 cells and also suppress the production of lymphocyte TNFα and INFγ in vitro .
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- HY-139807
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JAK
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Inflammation/Immunology
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JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16) .
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- HY-120604
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NVP_BVB808
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JAK
STAT
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Cancer
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BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of JAK2 and reduces the phosphorylation of STAT5, thereby blocking the JAK2-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research .
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- HY-161621
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JAK
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Inflammation/Immunology
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JAK-IN-37 (Compound WU4) is a JAK inhibitor, with IC50 values of 0.52, 2.26, 84 and 1.09 nM for JAK1, JAK2, JAK3 and JAK4, respectively. JAK-IN-37 can be used for the research of allogeneic hematopoietic cell transplantation (allo-HCT) .
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- HY-10961
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CYT387
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JAK
Autophagy
Apoptosis
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Cancer
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Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
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- HY-14435
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JAK
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Cancer
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Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
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- HY-143444
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JAK
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Inflammation/Immunology
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JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo .
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- HY-15315A
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LY3009104 phosphate; INCB028050 phosphate
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JAK
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Inflammation/Immunology
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Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
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- HY-12469
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VX-509; VRT-831509
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JAK
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Inflammation/Immunology
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Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.
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- HY-169242
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- HY-154994
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JAK
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Inflammation/Immunology
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JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor with IC50 values of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. JAK-IN-30 has research potential for dry eye disease (DED) .
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- HY-149296
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JAK
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Inflammation/Immunology
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JAK1-IN-12 is a selective inhibitor of JAK1, with IC50 of 0.0246 μM. And IC50s of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2. JAK1-IN-12 promotes hair growth in mice. JAK1-IN-12 can be used for research of immune and inflammatory diseases .
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- HY-151256
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JAK
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Cancer
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JAK-2/3-IN-2 (Compound 3h) is a JAK2 and JAK3 inhibitor with IC50s of 23.85 nM and 18.9 nM, respectively .
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- HY-130247B
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jak2/FLT3-IN-1 monomaleate
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JAK
FLT3
Apoptosis
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Cancer
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Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity .
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- HY-149283
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JAK
HDAC
Apoptosis
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Cancer
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JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
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- HY-161015
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JAK
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Inflammation/Immunology
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JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM. JAK1-IN-13 significantly decreases STAT3 phosphorylation .
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- HY-162248
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JAK
Interleukin Related
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Inflammation/Immunology
Cancer
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JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC50 values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC50s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a) .
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- HY-109053A
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JTE-052 ethanolate
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JAK
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Inflammation/Immunology
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Delgocitinib ethanolate is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .
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- HY-10962
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CYT387 sulfate salt
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JAK
Autophagy
Apoptosis
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Cancer
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Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
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- HY-145029
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- HY-153712
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-
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- HY-155951
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JAK
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Cancer
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JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor, with IC50 values of 38 and 600 nM for JAK3 and JAK2, respectively. JAK3-IN-14 shows inhibitory of IL-4 and IL-3 induced TF-1 cell proliferation, with IC50 values of 600 and 500 nM, respectively .
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- HY-163183
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JAK
Btk
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Inflammation/Immunology
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JAK3/BTK-IN-7 (XL-12) is a JAK3/BTK inhibitor with IC50 values of 2 nM and 14 nM, respectively. JAK3/BTK-IN-7 has anti-inflammatory activity and can be used in the study of rheumatoid arthritis .
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- HY-154969
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JAK
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Others
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JAK-IN-29 (compound 3) is a potent JAK inhibitor .
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- HY-157011
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- HY-143717
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JAK
Btk
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Inflammation/Immunology
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JAK3/BTK-IN-2 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)
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- HY-143720
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JAK
Btk
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Inflammation/Immunology
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JAK3/BTK-IN-5 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-5 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, example 35)
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- HY-143716
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JAK
Btk
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Inflammation/Immunology
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JAK3/BTK-IN-1 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002) .
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- HY-143718
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JAK
Btk
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Inflammation/Immunology
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JAK3/BTK-IN-3 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)
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- HY-143719
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JAK
Btk
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Inflammation/Immunology
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JAK3/BTK-IN-4 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-4 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 003)
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- HY-112724
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SHR0302
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
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- HY-112724A
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SHR0302 sulfate
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
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- HY-169326S
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JAK
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Cancer
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JAK2-IN-11 (Example 6) is a JAK2 kinase inhibitor with IC50 ≤10 nM against JH2 BIND WT/V617F. JAK2-IN-11 has antitumor activity .
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- HY-101976
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JAK
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Inflammation/Immunology
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JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
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- HY-153566
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JAK
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Cancer
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JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective JAK1 inhibitor .
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- HY-161684
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JAK
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Cancer
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JAK2-IN-10 (compound 5) is a potent JAK2 V617F inhibitor with an IC50 value of ≤10 nM .
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- HY-119935
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JAK
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Inflammation/Immunology
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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 .
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- HY-161019
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JAK
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Inflammation/Immunology
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JAK1/TYK2-IN-4 is a dual inhibitor of JAK and TYK2, with IC50s of 39 nM and 21 nM, respectively. JAK1/TYK2-IN-4 has oral bioavailability .
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- HY-109053
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JTE-052
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JAK
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Inflammation/Immunology
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Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .
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- HY-15508
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JANEX-1
4 Publications Verification
WHI-P131; jak3 inhibitor I
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JAK
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Cancer
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JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
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- HY-145336
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JAK
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Cancer
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JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 (IC50 = 29 and 41 nM respectively).
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- HY-100849
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JAK
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Inflammation/Immunology
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JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for autoimmune disease research .
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- HY-161967
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FLT3
JAK
Apoptosis
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Cancer
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JAK2/FLT3-IN-3 (11r) is a dual FLT3 and JAK2 inhibitor, with IC50 values of 2.01 nM, 0.51 nM and 104.40 nM for JAK2, FLT3 and JAK3, respectively. JAK2/FLT3-IN-3 (11r) induces apoptosis and possesses antitumor activity .
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- HY-156706
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JAK
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Cancer
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JAK-IN-31 (Example 75) is a JAK inhibitor with IC50 ranges of ≤0.01µM, ≤0.01µM, 0.01-0.1 µM and ≤0.01µM for JAK1, JAK2, JAK3 and Tyk2 respectively. JAK-IN-31 can be used in cancer research .
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- HY-130247
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jak2/FLT3-IN-1
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JAK
FLT3
Apoptosis
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Cancer
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Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib has anti-cancer activity .
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- HY-130247C
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jak2/FLT3-IN-1 sulfate
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JAK
FLT3
Apoptosis
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Cancer
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Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib maleate has anti-cancer activity .
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- HY-13577
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PF-03394197
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JAK
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Inflammation/Immunology
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Oclacitinib is a novel JAK inhibitor. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM).
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- HY-131906
-
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JAK
FLT3
Apoptosis
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Cancer
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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- HY-18300S
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GLPG0634-d4
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JAK
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Cancer
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Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
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- HY-128450
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- HY-117810
-
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JAK
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Inflammation/Immunology
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JAK2-IN-1 (eExample 2) is a JAK2 inhibitor, and can be used for research of proliferative disease, inflammatory disease, or renal disease .
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- HY-147754
-
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Btk
JAK
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Inflammation/Immunology
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JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research .
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- HY-46262
-
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JAK
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Cancer
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JAK-IN-15 is a JAK inhibitor. WO2016119700A1 (Compound 15) .
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- HY-50859
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INCB018424 sulfate
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JAK
Autophagy
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Cancer
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Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
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- HY-150688
-
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JNK
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Cancer
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JAK3-IN-13 (compound 12n) is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity .
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- HY-19568
-
ASP015K; JNJ-54781532
|
JAK
|
Inflammation/Immunology
|
Peficitinib (ASP015K) is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .
|
-
- HY-19568B
-
ASP015K hydrochloride; JNJ-54781532 hydrochloride
|
JAK
|
Inflammation/Immunology
|
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .
|
-
- HY-130247A
-
jak2/FLT3-IN-1 TFA
|
JAK
FLT3
Apoptosis
|
Cancer
|
Flonoltinib TFA is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib TFA has anti-cancer activity .
|
-
- HY-143884
-
|
JAK
|
Inflammation/Immunology
|
JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity .
|
-
- HY-13775
-
XL019
5 Publications Verification
|
JAK
Apoptosis
|
Cancer
|
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
|
-
- HY-151262
-
|
JAK
STING
NF-κB
STAT
|
Inflammation/Immunology
|
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD) .
|
-
- HY-100895
-
|
JAK
|
Cancer
|
SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
|
-
- HY-U00390
-
|
JAK
|
Cancer
|
JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
|
-
- HY-19568A
-
ASP015K hydrobromide; JNJ-54781532 hydrobromide
|
JAK
|
Inflammation/Immunology
|
Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .
|
-
- HY-14986
-
|
JAK
|
Others
|
JAK-IN-32 (XC) is a bi-aryl meta-pyrimidine inhibitor of JAK kinase .
|
-
- HY-143885
-
|
JAK
|
Inflammation/Immunology
|
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells .
|
-
- HY-15312
-
|
STAT
JAK
Apoptosis
|
Cancer
|
WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
|
-
- HY-139423
-
-
- HY-163653
-
|
JAK
|
Cancer
|
Zemprocitinib (Compound 1) is a Janus kinase (JAK) inhibitor. The IC50 values for JAK1, JAK2 and TYK2 are 5.95, 141.3 and 119 nM, respectively .
|
-
- HY-16997
-
INCB039110
|
JAK
|
Cancer
|
Itacitinib (INCB039110) is an orally active and selective inhibitor of JAK1 with an IC50 of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis .
|
-
- HY-101024
-
|
JAK
|
Inflammation/Immunology
|
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively .
|
-
- HY-14722A
-
|
JAK
|
Cancer
|
NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-14722C
-
|
JAK
|
Cancer
|
NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-14722
-
|
JAK
|
Cancer
|
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively .
|
-
- HY-111749
-
-
- HY-153702
-
|
JAK
|
Cancer
|
JAK-IN-27 (compound 1) is an orally active and potent JAKS family kinase inhibitor with IC50s of 3.0 nM (TYK2), 7.7 nM (JAK1), 629.6 nM (JAK3), respectively. JAK-IN-27 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=23.7 nM) .
|
-
- HY-169290
-
|
JAK
HDAC
|
Inflammation/Immunology
|
JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC50 values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity .
|
-
- HY-138222
-
WHI-P131 hydrochloride; jak3 inhibitor I hydrochloride
|
JAK
|
Cancer
|
JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3 inhibitor (Ki=2.3 μM). JANEX-1 hydrochloride shows potent JAK3 inhibitory activity (IC50=78 μM), does not inhibit JAK1 and JAK2 .
|
-
- HY-12000
-
Tyrphostin AG490; Tyrphostin B42
|
EGFR
STAT
JAK
Autophagy
|
Cancer
|
AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
|
-
- HY-148060
-
|
JAK
|
Cancer
|
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively .
|
-
- HY-152080
-
|
JAK
|
Inflammation/Immunology
|
TUL01101 is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. TUL01101 can be used for the research of rheumatoid arthritis .
|
-
- HY-18300R
-
|
JAK
|
Cancer
|
Filgotinib (Standard) is the analytical standard of Filgotinib. This product is intended for research and analytical applications. Filgotinib (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
|
-
- HY-112391
-
|
JAK
STAT
|
Cancer
|
SD-1029 is a JAK2/STAT3 inhibitor . SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation .
|
-
- HY-107361
-
AZD4205
|
JAK
|
Cancer
|
Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM) .
|
-
- HY-111471
-
-
- HY-18301
-
|
JAK
|
Cancer
|
JAK-IN-35 (compound TG46) is a JAK2 inhibitor that canb be used in cancer research .
|
-
- HY-108342
-
|
JAK
|
Inflammation/Immunology
|
PF-00956980 is a reversible pan-JAK inhibitor with IC50 values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases .
|
-
- HY-15270
-
|
JAK
|
Cancer
|
BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).
|
-
- HY-50856
-
Ruxolitinib
Maximum Cited Publications
147 Publications Verification
INCB18424
|
JAK
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
|
-
- HY-19631A
-
NS-018
|
JAK
|
Cancer
|
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-19631B
-
NS-018 hydrochloride
|
JAK
|
Cancer
|
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-19631
-
NS-018 maleate
|
JAK
|
Cancer
|
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
|
-
- HY-111471A
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283 .
|
-
- HY-149284
-
|
JAK
HDAC
|
Cancer
|
JAK/HDAC-IN-3 (13a) is a dual JAK and HDAC inhibitor, with IC50 values of 25.36 nM, 0.2 μM and 0.43 μM for JAK2, HDAC and HDAC1, respectively .
|
-
- HY-102046
-
FM-381
1 Publications Verification
|
JAK
|
Inflammation/Immunology
|
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
|
-
- HY-U00277
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-10 is a JAK inhibitor. JAK-IN-10 can be used for the research of dry eye disorders . JAK-IN-10 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-131194
-
|
Interleukin Related
|
Cancer
|
JAK2/STAT3-IN-1 (compound (S)-10a) is a potent GP130 inhibitor with an IC50 of 3.04 µM. JAK2/STAT3-IN-1 shows anti-tumor activity .
|
-
- HY-131140
-
BD750
4 Publications Verification
|
JAK
STAT
|
Inflammation/Immunology
Cancer
|
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively .
|
-
- HY-162862
-
|
JAK
|
Others
|
JAK-IN-38 (Compound 1) is a JAK inhibitor, with IC50s of 0.03, 0.06, 0.12, 0.44 μM for Tyk2, JAK3, JAK2, JAK1 respectively. JAK-IN-38 is a collagen VII (C7) inducer and has anti-inflammatory activity. JAK-IN-38 can upregulate the expression of COL7A1 mRNA in donor-derived keratinocytes and works together with Gentamicin (HY-A0276A) to boost overall C7 levels .
|
-
- HY-144058
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1) .
|
-
- HY-161259
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC50 value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases .
|
-
- HY-13577A
-
PF-03394197 monomaleate
|
JAK
|
Inflammation/Immunology
|
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
|
-
- HY-N1405
-
Elatericin B; JSI-124; NSC-521777
|
STAT
JAK
|
Cancer
|
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-40354
-
-
- HY-10410
-
|
FLT3
JAK
RET
Autophagy
Apoptosis
|
Cancer
|
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
|
-
- HY-144057
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-17 is a potent inhibitor of JAK. JAK-IN-17 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2021185305A1, compound 9-1) .
|
-
- HY-19568R
-
|
JAK
|
Inflammation/Immunology
|
Peficitinib (Standard) is the analytical standard of Peficitinib. This product is intended for research and analytical applications. Peficitinib (ASP015K) is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .
|
-
- HY-W064657
-
|
JAK
|
Others
|
Momelotinib (dihydrochloride) is a JAK1/JAK2 inhibitor that also antagonizes ACVR1, leading to downregulation of Hepcidin expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis .
|
-
- HY-153701
-
|
JAK
|
Cancer
|
JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM) .
|
-
- HY-50858
-
INCB018424 phosphate
|
JAK
Autophagy
Mitophagy
|
Cancer
|
Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
|
-
- HY-120469
-
|
JAK
|
Inflammation/Immunology
|
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively .
|
-
- HY-10409
-
TG-101348; SAR 302503
|
JAK
Apoptosis
|
Cancer
|
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-10409A
-
TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
|
JAK
Apoptosis
|
Cancer
|
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-112708
-
PF-06700841
|
JAK
|
Inflammation/Immunology
|
Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively .
|
-
- HY-151258
-
|
JAK
|
Cancer
|
TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research .
|
-
- HY-151259
-
|
JAK
|
Cancer
|
TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research .
|
-
- HY-50856R
-
|
JAK
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
Ruxolitinib (Standard) is the analytical standard of Ruxolitinib. This product is intended for research and analytical applications. Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
|
-
- HY-123099
-
|
JAK
|
Cancer
|
MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling .
|
-
- HY-124858
-
|
STAT
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities .
|
-
- HY-156423
-
|
Microtubule/Tubulin
JAK
|
Cancer
|
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells .
|
-
- HY-112708A
-
PF-06700841 P-Tosylate
|
JAK
|
Inflammation/Immunology
|
Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively .
|
-
- HY-167839
-
|
Apoptosis
|
Cancer
|
(R)-JAK2/STAT3-IN-1 is a GP130 D1 domain inhibitor with anti-tumor activity. (R)-JAK2/STAT3-IN-1 can inhibit the phosphorylation of JAK2 and STAT3. The affinity of (R)-JAK2/STAT3-IN-1 for GP130 protein is 3.8 μM. (R)-JAK2/STAT3-IN-1 effectively inhibits the viability and migration of tumor cells and promotes apoptosis .
|
-
- HY-18960
-
CHZ868
5 Publications Verification
|
JAK
|
Cancer
|
CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
|
-
- HY-123289
-
|
JAK
|
Inflammation/Immunology
|
CP-690550A is an analogue of Tofacitinib (HY-40354). CP-690550A is a dual inhibitor of JAK2 and JAK3 .
|
-
- HY-131014
-
|
JAK
|
Inflammation/Immunology
|
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases . FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
|
-
- HY-50856S2
-
INCB18424-d9
|
Isotope-Labeled Compounds
Apoptosis
JAK
Autophagy
Mitophagy
|
Cancer
|
Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
|
-
- HY-153050
-
|
JAK
|
Inflammation/Immunology
Cancer
|
JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM . JAK-IN-24 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-162031
-
|
JAK
|
Metabolic Disease
|
MMT3-72-M2 is an MMT3-72 metabolite. MMT3-72-M2 is a selective JAK1 inhibitor. MMT3-72-M2 inhibits JAK1, JAK2, TYK2, and JAK3 with IC50 values of 10.8 nM, 26.3 nM, 91.6 nM, 328.7 nM, respectlly .
|
-
- HY-156273
-
|
Apoptosis
HDAC
Epigenetic Reader Domain
JAK
|
Cancer
|
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo .
|
-
- HY-168269
-
|
JAK
|
Cancer
|
Tyk2-IN-20 (Example 289) is a potent Tyk2 inhibitor with an IC50 of <5 nM. Tyk2-IN-20 als inhibits JAK1, JAK2, and JAK3 with IIC50 values of <100 nM. Tyk2-IN-20 can be used for the study of inflammatory diseases .
|
-
- HY-P10840
-
|
JAK
MHC
|
Inflammation/Immunology
|
Tkip is a JAK2 specific inhibitor. Tkip can bind the JAK2 autophosphorylation site, inhibit the JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1. Tkip inhibits the antiviral activity of IFN-γ and the expression of MHC Class I molecules. Tkip can be used to study the IFN-γ signaling pathway .
|
-
- HY-18300
-
GLPG0634
|
JAK
HIV
|
Cancer
|
Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease .
|
-
- HY-18300A
-
GLPG0634 maleate
|
JAK
HIV
|
Inflammation/Immunology
|
Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease .
|
-
- HY-149718
-
|
JAK
HDAC
|
Cancer
|
Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models .
|
-
- HY-148785
-
|
JAK
|
Others
|
Nimucitinib is a Janus kinase (JAK) inhibitor .
|
-
- HY-16755
-
GSK-2586184; GLPG-0778
|
JAK
|
Inflammation/Immunology
|
Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
|
-
- HY-11067
-
WHI-P97
2 Publications Verification
|
JAK
|
Inflammation/Immunology
|
WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo .
|
-
- HY-10193
-
|
JAK
|
Cancer
|
AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively .
|
-
- HY-15315
-
LY3009104; INCB028050
|
JAK
|
Inflammation/Immunology
|
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-10193A
-
|
JAK
|
Cancer
|
(1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor .
|
-
- HY-18009
-
|
Btk
Polo-like Kinase (PLK)
JAK
|
Cancer
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
|
-
- HY-161354
-
|
JAK
Apoptosis
|
Inflammation/Immunology
|
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .
|
-
- HY-13450
-
|
JAK
EGFR
|
Inflammation/Immunology
|
ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3 .
|
-
- HY-108264
-
NIBR3049
|
JAK
PKC
GSK-3
|
Cancer
|
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively .
|
-
- HY-10409S
-
TG-101348-d9; SAR 302503-d9
|
Isotope-Labeled Compounds
Apoptosis
JAK
|
Cancer
|
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
|
-
- HY-40354A
-
-
- HY-122101
-
|
JAK
Apoptosis
|
Cancer
|
NSC114792 is a selective JAK3 inhibitor. NSC114792 induces apoptosis. NSC114792 decreases the protein expression of p-JAK3 and p-STAT5 .
|
-
- HY-103018
-
ASN-002
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-103018A
-
ASN-002 hydrochloride
|
JAK
Syk
|
Inflammation/Immunology
Cancer
|
Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
|
-
- HY-115452
-
|
JAK
Apoptosis
|
Cancer
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study .
|
-
- HY-N1356
-
-
- HY-40354S
-
Tasocitinib-13C3; CP-690550-13C3
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Tofacitinib- 13C3 is the 13C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
|
-
- HY-149647
-
-
- HY-107429
-
PF-04965842
|
JAK
|
Inflammation/Immunology
|
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
|
-
- HY-107595
-
|
JAK
STAT
Apoptosis
|
Cancer
|
SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway .
|
-
- HY-164393
-
|
JAK
Bcr-Abl
Apoptosis
|
Cancer
|
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
|
-
- HY-15999
-
PRT062070; PRT2070
|
JAK
Syk
|
Cancer
|
Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
|
-
- HY-158692
-
|
JAK
|
Cancer
|
Tyk2-IN-18 (compound 86) is a potent tyrosine kinase 2 (Tyk2) inhibitor. Tyk2-IN-18 inhibits JAK2-JH2, with an IC50 of <10 nM .
|
-
- HY-50856S
-
CTP-543; Ruxolitinib d8; Deuterated Ruxolitinib
|
JAK
|
Inflammation/Immunology
|
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata .
|
-
- HY-40354R
-
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Tofacitinib (Standard) is the analytical standard of Tofacitinib. This product is intended for research and analytical applications. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
|
-
- HY-148791
-
-
- HY-118084
-
Tyrene CR-4
|
JAK
Bcr-Abl
FLT3
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies .
|
-
- HY-123187
-
|
JAK
|
Cardiovascular Disease
|
AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat T cells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants .
|
-
- HY-U00318
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-11 is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment . JAK-IN-11 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15315S
-
LY3009104-d5; INCB028050-d5
|
JAK
|
Inflammation/Immunology
|
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-15315S1
-
LY3009104-d3; INCB028050-d3
|
JAK
|
Inflammation/Immunology
|
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-N1405R
-
Elatericin B (Standard); JSI-124 (Standard); NSC-521777 (Standard)
|
STAT
JAK
|
Cancer
|
Cucurbitacin I (Standard) is the analytical standard of Cucurbitacin I. This product is intended for research and analytical applications. Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-18228
-
|
JAK
|
Inflammation/Immunology
|
CP-352664 is a JAK inhibitor. CP-352664 has a inhibitoinhibits JAK3 with an EC50 value of 210 nM. CP-352664 is promising for research of organ transplant rejection and autoimmune disorders such as rheumatoid arthritis .
|
-
- HY-170393
-
|
JAK
STAT
|
Cancer
|
iBFAR2, a BFAR inhibitor, restores the CD8+ TRM cell subset against solid tumors. iBFAR2 promotes JAK2-STAT1 association and STAT1 phosphorylation .
|
-
- HY-10411
-
-
- HY-112442
-
|
JAK
|
Cancer
|
AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
|
-
- HY-109182
-
JNJ-64251330
|
JAK
|
Inflammation/Immunology
|
Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease .
|
-
- HY-107594
-
|
JAK
|
Cancer
|
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.
|
-
- HY-100544
-
FLLL32
5 Publications Verification
|
STAT
JAK
Apoptosis
|
Cancer
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells .
|
-
- HY-18293
-
|
JAK
Autophagy
|
Cancer
|
NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM .
|
-
- HY-139837
-
-
- HY-N1447
-
-
- HY-107429R
-
|
JAK
|
Inflammation/Immunology
|
Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
|
-
- HY-147330
-
|
PROTACs
JAK
|
Cancer
|
SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 can be used for the research of leukemia .
|
-
- HY-15315R
-
|
JAK
|
Inflammation/Immunology
|
Baricitinib (Standard) is the analytical standard of Baricitinib. This product is intended for research and analytical applications. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-132819
-
LY-3411067
|
JAK
|
Others
|
Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1) .
|
-
- HY-109179A
-
TP-0184 (hydrocholide)
|
JAK
TGF-β Receptor
|
Cancer
|
Itacnosertib hydrocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5 .
|
-
- HY-126242S
-
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].
|
-
- HY-19569
-
ABT-494
|
JAK
|
Inflammation/Immunology
|
Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research .
|
-
- HY-19569A
-
ABT-494 tartrate tetrahydrate
|
JAK
|
Inflammation/Immunology
|
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research .
|
-
- HY-168339
-
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, JAK1, and JAK3 with IC50s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .
|
-
- HY-N2959
-
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- HY-108419
-
|
JNK
|
Cancer
|
WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM .
|
-
- HY-40354AS
-
-
- HY-15166B
-
(E/Z)-TG02 citrate; (E/Z)-SB1317 citrate
|
CDK
JAK
FLT3
|
Cancer
|
(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor .
|
-
- HY-50514
-
AT9283
5 Publications Verification
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo .
|
-
- HY-107459
-
(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42
|
EGFR
STAT
JAK
|
Cancer
|
(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
|
-
- HY-147330A
-
|
PROTACs
JAK
|
Cancer
|
SJ1008030 (compound 8) TFA is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 TFA inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 TFA can be used for the research of leukemia .
|
-
- HY-147330B
-
|
PROTACs
JAK
|
Cancer
|
SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia .
|
-
- HY-144075
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8) .
|
-
- HY-170586
-
-
- HY-100754
-
PF-06651600
|
JAK
|
Inflammation/Immunology
|
Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM .
|
-
- HY-121874
-
|
JAK
|
Cancer
|
EP009 is a JAK3 inhibitor that selectively inhibits IL-2-mediated JAK3 tyrosine phosphorylation (IC50=10-20 μM in Kit225 cells) without affecting IL-3-induced JAK2 phosphorylation (up to 50 μM in BaF/3 cells). EP009 significantly reduced Kit225 cell viability (72 h, LD50=5.0 μM) while having no effect on BaF/3 cells. .
|
-
- HY-N13294
-
TMJ-105
|
Apoptosis
JAK
STAT
p38 MAPK
JNK
ERK
|
Cancer
|
Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC50 value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy .
|
-
- HY-10058
-
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo .
|
-
- HY-40354AR
-
|
JAK
Apoptosis
Bacterial
Fungal
Influenza Virus
|
Infection
Inflammation/Immunology
Cancer
|
Tofacitinib (citrate) (Standard) is the analytical standard of Tofacitinib (citrate). This product is intended for research and analytical applications. Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
|
-
- HY-151385
-
|
JAK
STAT
IFNAR
Interleukin Related
|
Cancer
|
VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146066A
-
|
Others
|
Others
|
(R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
- HY-169758
-
|
JAK
|
Inflammation/Immunology
|
CEE321 is a potent pan-JAK inhibitor with an IC50 value of 54 nM. CEE321 potently inhibits biomarkers associated with atopic dermatitis .
|
-
- HY-15343
-
|
JAK
|
Cancer
|
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
|
-
- HY-111077
-
|
JAK
STAT
|
Inflammation/Immunology
Cancer
|
INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma .
|
-
- HY-16379
-
SB1518
|
JAK
FLT3
|
Cancer
|
Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
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- HY-146066
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nAChR
JAK
STAT
NO Synthase
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Inflammation/Immunology
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α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
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- HY-149257
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JAK
STAT
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Cancer
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HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions .
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- HY-109175
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JAK
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Inflammation/Immunology
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Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases .
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- HY-151385A
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STAT
Interleukin Related
IFNAR
JAK
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Cancer
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(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . (R,R)-VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-19569R
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ABT-494 (Standard)
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JAK
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Inflammation/Immunology
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Upadacitinib (Standard) is the analytical standard of Upadacitinib. This product is intended for research and analytical applications. Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research .
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- HY-18200A
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E5555 hydrochloride; ER-172594-00 hydrochloride
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Protease Activated Receptor (PAR)
JAK
Apoptosis
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Cardiovascular Disease
Cancer
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Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
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- HY-15999A
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PRT062070 hydrochloride; PRT2070 hydrochloride
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Syk
JAK
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Cancer
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Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies .
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- HY-N2959R
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JAK
STAT
Apoptosis
Autophagy
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Cancer
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Brevilin A (Standard) is the analytical standard of Brevilin A. This product is intended for research and analytical applications. Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
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- HY-12589
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JAK
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Neurological Disease
Cancer
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ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
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- HY-12589A
-
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JAK
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Neurological Disease
Cancer
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ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
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- HY-N3710
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Kumujian G; O-Methylpicrasidine I
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JAK
Apoptosis
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Neurological Disease
Cancer
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Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain .
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- HY-156621
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JAK
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Inflammation/Immunology
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Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases .
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- HY-40354B
-
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JAK
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Inflammation/Immunology
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(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
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- HY-40354D
-
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JAK
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Inflammation/Immunology
|
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
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- HY-15166A
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(E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride
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CDK
JAK
FLT3
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Cancer
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(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor .
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- HY-100754C
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PF-06651600 tosylate
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JAK
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Inflammation/Immunology
|
Ritlecitinib tosylate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. Ritlecitinib tosylate is used for inflammatory and autoimmune diseases research .
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- HY-125019
-
|
JAK
STAT
|
Inflammation/Immunology
|
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) .
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- HY-144031S
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-
- HY-N2963
-
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ERK
p38 MAPK
JAK
STAT
TNF Receptor
Interleukin Related
COX
Arginase
|
Inflammation/Immunology
|
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis .
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- HY-164455
-
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Aurora Kinase
JAK
STAT
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Inflammation/Immunology
|
AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
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- HY-50856A
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S-Ruxolitinib; S-INCB18424
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JAK
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Cancer
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Ruxolitinib (S enantiomer) (S-Ruxolitinib) is the S-enantiomer of Ruxolitinib (HY-50856). Ruxolitinib (S enantiomer) is an orally active, potent JAK inhibitor .
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- HY-16997A
-
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JAK
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Cancer
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Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
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- HY-40354C
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