Search Result
Results for "
Tyk2 inhibitor
" in MedChemExpress (MCE) Product Catalog:
12
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-144031S
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- HY-161683
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JAK
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Neurological Disease
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Tyk2-IN-19 (Compound 1) is an orally active and blood-brain barrier (BBB) permeable Tyk2 inhibitor. Tyk2-IN-19 can be used for study of neurodegenerative diseases .
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- HY-163303
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JAK
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Inflammation/Immunology
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Tyk2-in-15 (Compound 97) is a selective tyrosine kinase 2 (Tyk2) inhibitor with IC50 value ≤ 10 nM for Tyk2-JH2. Tyk2-IN-15 can be used in the study of inflammatory or autoimmune diseases .
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- HY-163304
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JAK
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Cancer
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Tyk2-IN-16 is a selective and potent TYK2 inhibitor with an IC50 of <10 nM for TYK2-JH2. Tyk2-IN-16 inhibits pSTAT4 with an IC50 of <10 nM in NK92 cells (WO2023220046A1; compound 184) .
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- HY-168269
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JAK
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Cancer
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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 .
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- HY-18709
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- HY-169984S
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Isotope-Labeled Compounds
STAT
JAK
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Inflammation/Immunology
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Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). 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 .
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- HY-163305
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- HY-168339
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JAK
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Inflammation/Immunology
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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 .
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- HY-143884
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JAK
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Inflammation/Immunology
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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 .
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- HY-111745
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JAK
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Inflammation/Immunology
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Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis .
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- HY-101762
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JAK
Phosphodiesterase (PDE)
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Inflammation/Immunology
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TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases .
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- HY-126242S
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JAK
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Inflammation/Immunology
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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 .
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- HY-158692
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JAK
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Cancer
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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 .
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- HY-144032
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JAK
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Inflammation/Immunology
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Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease .
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- HY-144087
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JAK
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Inflammation/Immunology
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TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease .
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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-150720
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JAK
IFNAR
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Inflammation/Immunology
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TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research .
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- HY-163312S
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JAK
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Inflammation/Immunology
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Tyk2-IN-18-d5 (Compound 13) is the deuterated TYK2 inhibitor, targeting to JH2 domain. Tyk2-IN-18-d5 can be used for the research of inflammatory and autoimmune diseases .
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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-163314S
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- HY-150096
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NDI-034858; TAK-279
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JAK
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Inflammation/Immunology
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Zasocitinib (NDI-034858) is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM .
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- HY-172596
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JAK
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Inflammation/Immunology
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TYK2 activator-1 (16b) is a TYK2 activator with anEC50 of 1.78 μM. TYK2 activator-1 inhibits JAK2 and JAK3 with the IC50 values of 6.8 and 6.3 μM, respectively .
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- HY-143885
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JAK
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Inflammation/Immunology
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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 .
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- HY-149892S
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JAK
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Cancer
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TYK2?JH2-IN-1-d3 is the a deuterated, orally active and selective TYK2 inhibitor (compound 4h), targeting to JH2 domain (IC50=0.1 nM) .
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- HY-156409
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JAK
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Inflammation/Immunology
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ABBV-712 is a selective and orally active inhibitor of Tyrosine kinase 2 (TYK2). ABBV-712 has EC50 values of 0.01, 0.19, and 0.17 μM for TYK2 JH2, TYK2 cells and human whole blood, respectively. ABBV-712 has anti-inflammatory activity and can be used in the research of autoimmune diseases .
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- HY-120469
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JAK
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Inflammation/Immunology
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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 .
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- HY-138317
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JAK
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Cancer
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Tyk2-IN-10 (compound 17.5) is a tyrosine kinase 2-mediated signaling inhibitor involved in inflammation regulation .
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- HY-160144S
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- HY-117287
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BMS-986165
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JAK
Interleukin Related
IFNAR
Isotope-Labeled Compounds
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Inflammation/Immunology
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Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .
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- HY-18316
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- HY-156466
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STAT
Interleukin Related
IFNAR
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Inflammation/Immunology
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QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC50=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC50=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE) .
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- HY-160144S2
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(rac)-BMS-986322
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Drug Isomer
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Others
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(rac)-Lomedeucitinib ((rac)-BMS-986322) is the racemate of Lomedeucitinib. Lomedeucitinib (BMS-986322) is a tyrosine protein kinase (TYK2) inhibitor. Lomedeucitinib has anti-inflammatory activity and significant inhibitory effect on IFNα (IC50=0.047 μM) production downstream of IL-12/TYK2. Lomedeucitinib is indicated for the study of plaque psoriasis and pruritus .
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- HY-18710
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- HY-101024
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JAK
STAT
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Inflammation/Immunology
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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. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation .
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- HY-160144S1
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(S)-BMS-986322
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JAK
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Inflammation/Immunology
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(S)-Lomedeucitinib ((S)-BMS-986322) is a S-enantiomer of Lomedeucitinib (HY-160144S). Lomedeucitinib is a tyrosine protein kinase (TYK2) inhibitor .
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- HY-16640
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JAK
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Inflammation/Immunology
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TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD) .
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- HY-100895
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JAK
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Cancer
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SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
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- HY-163653
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JAK
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Cancer
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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 .
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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-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-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-15270
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JAK
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Cancer
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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).
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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-13034
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LY2784544
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JAK
FLT3
FGFR
VEGFR
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Cancer
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Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
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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-173357
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PROTACs
JAK
STAT
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Inflammation/Immunology
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TYD-68 is a highly efficient and selective CRBN-recruited TYK2 PROTAC degrader with a DC50 value of 0.42 nM. TYD-68 significantly inhibits IL-12 and IFN-α-induced STAT4 and STAT1 phosphorylation, thereby blocking TYK2-dependent signaling pathways.
TYD-68 can be used in the study of psoriasis. (Pink: Target protein ligand (HY-173359); Black: Linker (HY-W007732B); Blue: E3 ligase ligand (HY-14658); E3 ligase ligand + Linker (HY-173358)) .
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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-19568B
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ASP015K hydrochloride; JNJ-54781532 hydrochloride
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JAK
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Inflammation/Immunology
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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 .
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- HY-19568
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ASP015K; JNJ-54781532
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JAK
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Inflammation/Immunology
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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 .
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- HY-131968
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JAK
Cytochrome P450
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Inflammation/Immunology
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BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
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- HY-15999
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PRT062070; PRT2070
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JAK
Syk
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Cancer
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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.
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- HY-19568A
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ASP015K hydrobromide; JNJ-54781532 hydrobromide
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JAK
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Inflammation/Immunology
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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 .
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- HY-18315
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JAK
Apoptosis
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Cancer
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Bayer-18 is an inhibitor for TYK2. Bayer-18 inhibits the viability of ALCL cell K299, SR786, Mac1 and Mac2a with IC50 of 2-3 µM, and induces apoptosis in K299 and SR786 .
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- HY-148060
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JAK
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Cancer
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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 .
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- HY-18300R
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JAK
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Cancer
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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.
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- HY-152080
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JAK
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Inflammation/Immunology
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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 .
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- HY-16755
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GSK-2586184; GLPG-0778
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JAK
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Inflammation/Immunology
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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.
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- HY-112708
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PF-06700841
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JAK
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Inflammation/Immunology
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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 .
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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-19631
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NS-018 maleate
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JAK
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Cancer
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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).
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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-19631B
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NS-018 hydrochloride
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JAK
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Cancer
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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).
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- HY-19631A
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NS-018
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JAK
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Cancer
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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).
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- HY-153058
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LRRK2
JAK
AMPK
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Neurological Disease
Cancer
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LRRK2-IN-8 is a LRRK2 inhibitor. LRRK2-IN-8 inhibits LRRK2 (wt) and LRRK2 (G2019) with IC50s lower than 10 nM, and inhibits TYK2 and NUAK1 with IC50s of 10-100 nM .
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- HY-102046
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FM-381
1 Publications Verification
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JAK
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Inflammation/Immunology
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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.
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- HY-112708A
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PF-06700841 P-Tosylate
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JAK
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Inflammation/Immunology
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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 .
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- HY-19568R
-
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JAK
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Inflammation/Immunology
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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 .
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- HY-16997
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INCB039110
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JAK
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Cancer
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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 .
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- HY-14722C
-
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JAK
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Cancer
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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 .
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- HY-14722A
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JAK
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Cancer
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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-15999A
-
|
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
|
Cancer
|
|
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 .
|
-
- 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-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-171242
-
|
|
JAK
STAT
|
Others
|
|
LNK01004 is a JAK inhibitor with strong inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50:＜0.51 nM) and TYK2 (IC50: 1.0 nM) . LNK01004 can simultaneously inhibit multiple cytokine-induced p-STAT signaling pathways. LNK01004 can be used in the research of diseases such as atopic dermatitis .
|
-
- HY-156961
-
|
|
JAK
|
Inflammation/Immunology
|
|
GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases .
|
-
- HY-156706
-
|
|
JAK
|
Cancer
|
|
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 .
|
-
- HY-153440
-
|
|
JAK
|
Cancer
|
|
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 .
|
-
- 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-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-100849
-
|
|
JAK
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-113787
-
|
|
Ack1
JAK
|
Cancer
|
|
(R)-9b is a potent inhibitor of ACK1 tyrosine kinase (IC50=56 nM) with anticancer activity. (R)-9b exhibits selectivity for ACK1 but has inhibitory effects on JAK family kinases JAK2 and Tyk2. (R)-9b can be used in the study of hormone-regulated cancers such as prostate and breast cancer .
|
-
- 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-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-149296
-
|
|
JAK
|
Inflammation/Immunology
|
|
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 .
|
-
- 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-112724
-
|
SHR0302
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-112724A
-
|
SHR0302 sulfate
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- 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-120604
-
|
NVP_BVB808
|
JAK
STAT
|
Cancer
|
|
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 .
|
-
- 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-117287A
-
|
BMS-986165 hydrochloride
|
Interleukin Related
JAK
IFNAR
|
Inflammation/Immunology
|
|
Deucravacitinib hydrochloride (BMS-986165 hydrochloride) is a highly selective all-site inhibitor with potent inhibitory activity against TYK2. Deucravacitinib hydrochloride can effectively block IL-12, IL-23 and type I interferon signaling. Deucravacitinib hydrochloride demonstrates significant efficacy in preclinical models of inflammatory bowel disease. Deucravacitinib hydrochloride demonstrated superiority over placebo and apremilast on multiple efficacy endpoints in moderate to severe plaque psoriasis. Deucravacitinib hydrochloride was well tolerated in inhibition .
|
-
- 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-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-150688
-
|
|
JNK
|
Cancer
|
|
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 .
|
-
- 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-170772
-
|
|
p38 MAPK
STAT
Interleukin Related
Cathepsin
JAK
|
Inflammation/Immunology
|
|
Dual Cathepsin L/JAK-IN-1 (Compound A8) is a dual inhibitor of Cathepsin L (CTSL) and JAK, with IC50 values of 0.68 μM, 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for CTSL, JAK1/2/3, and TYK2, respectively. Dual Cathepsin L/JAK-IN-1 effectively blocks the activation of the MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. Dual Cathepsin L/JAK-IN-1 can be used in research on acute lung injury (ALI) .
|
-
- HY-100754C
-
|
PF-06651600 tosylate
|
JAK
Interleukin Related
STAT
|
Inflammation/Immunology
|
|
Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .
|
-
- HY-100754
-
|
PF-06651600
|
JAK
Interleukin Related
STAT
|
Inflammation/Immunology
|
|
Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .
|
-
- HY-100754A
-
|
PF-06651600 (malonate)
|
JAK
Interleukin Related
STAT
|
Inflammation/Immunology
|
|
Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-144031S
-
|
|
|
Tyk2-IN-8 is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease .
|
-
-
- HY-126242S
-
|
|
|
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 .
|
-
-
- HY-160144S
-
|
|
|
Lomedeucitinib (BMS-986322) is a tyrosine protein kinase (TYK2) inhibitor .
|
-
-
- HY-117287
-
|
|
|
Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .
|
-
-
- HY-160144S2
-
|
|
|
(rac)-Lomedeucitinib ((rac)-BMS-986322) is the racemate of Lomedeucitinib. Lomedeucitinib (BMS-986322) is a tyrosine protein kinase (TYK2) inhibitor. Lomedeucitinib has anti-inflammatory activity and significant inhibitory effect on IFNα (IC50=0.047 μM) production downstream of IL-12/TYK2. Lomedeucitinib is indicated for the study of plaque psoriasis and pruritus .
|
-
-
- HY-160144S1
-
|
|
|
(S)-Lomedeucitinib ((S)-BMS-986322) is a S-enantiomer of Lomedeucitinib (HY-160144S). Lomedeucitinib is a tyrosine protein kinase (TYK2) inhibitor .
|
-
-
- HY-169984S
-
|
|
|
Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). 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-163312S
-
|
|
|
Tyk2-IN-18-d5 (Compound 13) is the deuterated TYK2 inhibitor, targeting to JH2 domain. Tyk2-IN-18-d5 can be used for the research of inflammatory and autoimmune diseases .
|
-
-
- HY-163314S
-
|
|
|
Tyk2-IN-18-d3 (Compound 18) is a Tyk2 inhibitor with an IC50 value of < 30 nM for both IL-23 and IFNα. Tyk2-IN-18-d3 can be used for research on autoimmune diseases .
|
-
-
- HY-149892S
-
|
|
|
TYK2?JH2-IN-1-d3 is the a deuterated, orally active and selective TYK2 inhibitor (compound 4h), targeting to JH2 domain (IC50=0.1 nM) .
|
-
-
- HY-18300S
-
|
|
|
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.
|
-
-
- HY-131968
-
|
|
|
BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-172596
-
|
|
|
Alkynes
|
|
TYK2 activator-1 (16b) is a TYK2 activator with anEC50 of 1.78 μM. TYK2 activator-1 inhibits JAK2 and JAK3 with the IC50 values of 6.8 and 6.3 μM, respectively .
|
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