Search Result
Results for "
JAK3 Inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-161354
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JAK
Apoptosis
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Inflammation/Immunology
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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 .
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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-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-149718
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JAK
HDAC
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Cancer
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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 .
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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, compound 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-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-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-150688
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JNK
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Cancer
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JAK3-IN-13 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-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-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-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-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-U00390
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JAK
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Cancer
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JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
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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-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-123099
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JAK
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Cancer
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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 .
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- HY-131140
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BD750
2 Publications Verification
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JAK
STAT
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Inflammation/Immunology
Cancer
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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 .
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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-108419
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JNK
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Cancer
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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 .
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- HY-131014
-
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JAK
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Inflammation/Immunology
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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.
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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-11067
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WHI-P97
2 Publications Verification
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JAK
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Inflammation/Immunology
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WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo .
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- HY-100754
-
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PF-06651600
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JAK
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Inflammation/Immunology
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Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM .
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- HY-40354
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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
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(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
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- HY-40354C
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JAK
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Inflammation/Immunology
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(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
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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-100754C
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PF-06651600 tosylate
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JAK
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Inflammation/Immunology
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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-13895
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EGFR
JAK
Apoptosis
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Cancer
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WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
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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-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-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-15312
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STAT
JAK
Apoptosis
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Cancer
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WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
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- HY-18300
-
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GLPG0634
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JAK
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Cancer
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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-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-100754A
-
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PF-06651600 (malonate)
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JAK
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Inflammation/Immunology
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Ritlecitinib (PF-06651600) malonate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. Ritlecitinib (malonate) can be used for the research of inflammatory and autoimmune diseases .
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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-40354S
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Tasocitinib-13C3; CP-690550-13C3
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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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.
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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-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-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-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-107361
-
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AZD4205
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JAK
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Cancer
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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) .
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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-50858
-
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INCB018424 phosphate
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JAK
Autophagy
Mitophagy
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Cancer
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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.
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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-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-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-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-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-151258
-
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JAK
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Cancer
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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 .
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- HY-151259
-
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JAK
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Cancer
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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 .
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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-101024
-
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JAK
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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 .
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- HY-18300A
-
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GLPG0634 maleate
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JAK
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Inflammation/Immunology
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Filgotinib (maleate) 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. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research .
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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-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-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-108342
-
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JAK
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Inflammation/Immunology
|
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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 .
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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-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-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-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-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-147741
-
|
|
JAK
Btk
EGFR
|
Inflammation/Immunology
Cancer
|
|
DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-154994
-
|
|
JAK
|
Inflammation/Immunology
|
|
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-50859
-
|
INCB018424 sulfate
|
JAK
Autophagy
|
Cancer
|
|
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-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 .
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-
- HY-100754B
-
|
(2R,5S)-PF-06651600
|
JAK
|
Inflammation/Immunology
|
|
(2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective JAK3 inhibitor (IC50=144.8 nM) extracted from patent US20150158864A1, example 68 .
|
-
- 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-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-146672
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
|
-
- 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-116505
-
|
|
JAK
|
Cancer
|
|
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) .
|
-
- 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-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-50856
-
Ruxolitinib
Maximum Cited Publications
121 Publications Verification
INCB18424
|
JAK
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
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-137756
-
|
|
JAK
|
Cancer
|
|
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 .
|
-
- 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-147742
-
|
|
JAK
|
Inflammation/Immunology
|
|
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-163267
-
|
|
Others
|
Others
|
|
ZNL0325 is a covalent probe based on pyrazolopyrimidine. ZNL0325 features an acrylamide side chain at the C3 position, which is capable of forming covalent bonds with multiple kinases that possess a cysteine at the αD-1 position, including BTK, EGFR, BLK, and JAK3. ZNL0325 can be used in the research of creating structurally distinct covalent kinase inhibitors .
|
-
- 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-18303
-
AMG-47a
2 Publications Verification
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
|
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity .
|
-
- 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-80002
-
|
BMX kinase Inhibitor
|
Btk
BMX Kinase
|
Cancer
|
|
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
|
-
- 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-130247
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-1 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 .
|
-
- 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-130247A
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
JAK2/FLT3-IN-1 (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. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity .
|
-
- 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-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-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-151285
-
|
|
Apoptosis
JAK
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- 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-18949
-
|
|
FLT3
JAK
c-Kit
|
Cancer
|
|
JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia .
|
-
- HY-111553
-
|
|
EGFR
|
Cancer
|
|
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors .
|
-
- HY-131906
-
|
|
JAK
FLT3
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-13775
-
XL019
4 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-109082
-
|
SKI-O-703
|
Syk
|
Inflammation/Immunology
|
|
Cevidoplenib (SKI-O-703) is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. Cevidoplenib is also the mesylate form of SKI-O-592. Cevidoplenib and SKI-O-592 inhibits BCR-mediated survival, proliferation, and differentiation of B cells. And SKI-O-592 potently inhibits multiple kinases with IC50s of 6.2 nM (Syk), 1.859 μM (Jak2), 5.807 μM (Jak3), 0.412 μM (RET), 0.687 μM (KOR), 1.783 μM (FLT3), 16.96 μM (FGFR1), 5.662 μM (FGFR3), and 0.709 μM (Pyk2), respectively .
|
-
- 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-147826
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
|
-
- 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-161618
-
|
|
JAK
EGFR
PI3K
IGF-1R
GSK-3
|
Inflammation/Immunology
Endocrinology
|
|
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in LPS‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
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-
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-40354S
-
|
|
|
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-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.
|
-
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