Search Result
Results for "
selective JAK inhibitor
" in MedChemExpress (MCE) Product Catalog:
10
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-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-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-153568
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JAK
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Cancer
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JAK1-IN-11 (compound 11) is a potent inhibitor of JAK,with IC50s of 0.02 nM (JAK1),and 0.44 nM (JAK2),respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2 .
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- HY-144440
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JAK
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Cancer
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JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC50 of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more .
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- HY-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-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-120604
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NVP_BVB808
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JAK
STAT
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Cancer
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BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of JAK2 and reduces the phosphorylation of STAT5, thereby blocking the JAK2-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research .
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- HY-50859
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INCB018424 sulfate
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JAK
Autophagy
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Cancer
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Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
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- HY-161139
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JAK
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Inflammation/Immunology
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JAK1-IN-14 (Compound 12a) is a potent and selective JAK1 inhibitor. JAK1-IN-14 inhibits JAK1 and JAK2 with an IC50 value of 12.6 nM and 135 nM. JAK1-IN-14 suppresses hepatic fibrosis levels and can be used for the research of liver fibrosis and inflammatory diseases .
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- HY-15315A
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LY3009104 phosphate; INCB028050 phosphate
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JAK
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Inflammation/Immunology
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Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
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- HY-10963
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CYT387 mesylate
|
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-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-116505
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JAK
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Cancer
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JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM) .
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- HY-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-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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-
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- HY-153566
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JAK
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Cancer
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JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective JAK1 inhibitor .
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-
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- HY-155746
-
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JAK
|
Infection
Inflammation/Immunology
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JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs) .
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- HY-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-137756
-
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JAK
|
Cancer
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JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells .
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- HY-128450
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-
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- HY-161015
-
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JAK
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Inflammation/Immunology
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JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM. JAK1-IN-13 significantly decreases STAT3 phosphorylation .
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- HY-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-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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-
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- HY-50856
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Ruxolitinib
Maximum Cited Publications
143 Publications Verification
INCB18424
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JAK
Autophagy
Mitophagy
Apoptosis
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Cancer
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Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
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- HY-131906
-
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JAK
FLT3
Apoptosis
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Cancer
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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- HY-10410
-
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FLT3
JAK
RET
Autophagy
Apoptosis
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Cancer
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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.
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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-133747
-
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JAK
|
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-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-N1405
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Elatericin B; JSI-124; NSC-521777
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STAT
JAK
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Cancer
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Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
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- HY-13775
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XL019
5 Publications Verification
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JAK
Apoptosis
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Cancer
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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 .
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- HY-149296
-
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JAK
|
Inflammation/Immunology
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JAK1-IN-12 is a selective inhibitor of JAK1, with IC50 of 0.0246 μM. And IC50s of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2. JAK1-IN-12 promotes hair growth in mice. JAK1-IN-12 can be used for research of immune and inflammatory diseases .
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- HY-101024
-
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JAK
|
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-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-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-10409
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TG-101348; SAR 302503
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JAK
Apoptosis
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Cancer
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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 .
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- HY-10409A
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TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate
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JAK
Apoptosis
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Cancer
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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 .
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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-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-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-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-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-50856R
-
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JAK
Autophagy
Mitophagy
Apoptosis
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Cancer
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Ruxolitinib (Standard) is the analytical standard of Ruxolitinib. This product is intended for research and analytical applications. Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
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- HY-112724
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SHR0302
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
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-
-
- HY-112724A
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SHR0302 sulfate
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
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Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
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-
- HY-161259
-
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JAK
|
Inflammation/Immunology
|
JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC50 value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases .
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-
-
- HY-19631A
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NS-018
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JAK
|
Cancer
|
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
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-
-
- HY-19631B
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NS-018 hydrochloride
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JAK
|
Cancer
|
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
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-
- HY-19631
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NS-018 maleate
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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).
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- HY-102046
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FM-381
1 Publications Verification
|
JAK
|
Inflammation/Immunology
|
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
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-
- HY-50856S2
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INCB18424-d9
|
Isotope-Labeled Compounds
Apoptosis
JAK
Autophagy
Mitophagy
|
Cancer
|
Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
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- HY-50858
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INCB018424 phosphate
|
JAK
Autophagy
Mitophagy
|
Cancer
|
Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
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- HY-120469
-
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JAK
|
Inflammation/Immunology
|
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively .
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- HY-108264
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NIBR3049
|
JAK
PKC
GSK-3
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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 .
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- HY-11067
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WHI-P97
2 Publications Verification
|
JAK
|
Inflammation/Immunology
|
WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo .
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- HY-15315
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LY3009104; INCB028050
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JAK
|
Inflammation/Immunology
|
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
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-
- HY-150688
-
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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 .
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- HY-112442
-
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JAK
|
Cancer
|
AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
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- HY-13450
-
|
JAK
EGFR
|
Inflammation/Immunology
|
ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3 .
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- HY-18293
-
|
JAK
Autophagy
|
Cancer
|
NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM .
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- HY-161354
-
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JAK
Apoptosis
|
Inflammation/Immunology
|
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .
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- HY-122101
-
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JAK
Apoptosis
|
Cancer
|
NSC114792 is a selective JAK3 inhibitor. NSC114792 induces apoptosis. NSC114792 decreases the protein expression of p-JAK3 and p-STAT5 .
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- HY-10409S
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TG-101348-d9; SAR 302503-d9
|
Isotope-Labeled Compounds
Apoptosis
JAK
|
Cancer
|
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
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- HY-124858
-
|
STAT
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities .
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- HY-15999
-
PRT062070; PRT2070
|
JAK
Syk
|
Cancer
|
Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
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-
- 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 .
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-
- HY-19569
-
ABT-494
|
JAK
|
Inflammation/Immunology
|
Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research .
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-
- HY-19569A
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ABT-494 tartrate tetrahydrate
|
JAK
|
Inflammation/Immunology
|
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research .
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- HY-131014
-
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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-15315S
-
LY3009104-d5; INCB028050-d5
|
JAK
|
Inflammation/Immunology
|
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-15315S1
-
LY3009104-d3; INCB028050-d3
|
JAK
|
Inflammation/Immunology
|
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-N1405R
-
Elatericin B (Standard); JSI-124 (Standard); NSC-521777 (Standard)
|
STAT
JAK
|
Cancer
|
Cucurbitacin I (Standard) is the analytical standard of Cucurbitacin I. This product is intended for research and analytical applications. Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-100754
-
PF-06651600
|
JAK
|
Inflammation/Immunology
|
Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM .
|
-
- HY-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-115452
-
|
JAK
Apoptosis
|
Cancer
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study .
|
-
- HY-15343
-
|
JAK
|
Cancer
|
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
|
-
- HY-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-147330
-
|
PROTACs
JAK
|
Cancer
|
SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 can be used for the research of leukemia .
|
-
- HY-15315R
-
|
JAK
|
Inflammation/Immunology
|
Baricitinib (Standard) is the analytical standard of Baricitinib. This product is intended for research and analytical applications. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-109175
-
|
JAK
|
Inflammation/Immunology
|
Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases .
|
-
- HY-U00318
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-11 is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment . JAK-IN-11 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100754C
-
PF-06651600 tosylate
|
JAK
|
Inflammation/Immunology
|
Ritlecitinib tosylate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. Ritlecitinib tosylate is used for inflammatory and autoimmune diseases research .
|
-
- HY-147330A
-
|
PROTACs
JAK
|
Cancer
|
SJ1008030 (compound 8) TFA is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 TFA inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 TFA can be used for the research of leukemia .
|
-
- HY-147330B
-
|
PROTACs
JAK
|
Cancer
|
SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 formic can be used for the research of leukemia .
|
-
- HY-19569R
-
ABT-494 (Standard)
|
JAK
|
Inflammation/Immunology
|
Upadacitinib (Standard) is the analytical standard of Upadacitinib. This product is intended for research and analytical applications. Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research .
|
-
- HY-16997A
-
|
JAK
|
Cancer
|
Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
|
-
- HY-111077
-
|
JAK
STAT
|
Inflammation/Immunology
Cancer
|
INCB16562 is an orally active and selective inhibitor against JAK1/2 markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma .
|
-
- HY-168339
-
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, JAK1, and JAK3 with IC50s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation .
|
-
- HY-126294
-
AZD4604; JAK1-IN-7
|
JAK
|
Inflammation/Immunology
|
Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity .
|
-
- 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-144075
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8) .
|
-
- HY-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-109148
-
TD-1473; JNJ-8398
|
JAK
|
Inflammation/Immunology
|
Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis .
|
-
- HY-151385
-
|
JAK
STAT
IFNAR
Interleukin Related
|
Cancer
|
VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-126242S
-
|
JAK
|
Inflammation/Immunology
|
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].
|
-
- HY-121874
-
|
JAK
|
Cancer
|
EP009 is a JAK3 inhibitor that selectively inhibits IL-2-mediated JAK3 tyrosine phosphorylation (IC50=10-20 μM in Kit225 cells) without affecting IL-3-induced JAK2 phosphorylation (up to 50 μM in BaF/3 cells). EP009 significantly reduced Kit225 cell viability (72 h, LD50=5.0 μM) while having no effect on BaF/3 cells. .
|
-
- HY-100754A
-
PF-06651600 (malonate)
|
JAK
|
Inflammation/Immunology
|
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 .
|
-
- HY-144031S
-
-
- HY-151385A
-
|
STAT
Interleukin Related
IFNAR
JAK
|
Cancer
|
(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . (R,R)-VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145588
-
INCB54707
|
JAK
|
Inflammation/Immunology
|
Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) .
|
-
- HY-144087
-
|
JAK
|
Inflammation/Immunology
|
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 .
|
-
- HY-144032
-
|
JAK
|
Inflammation/Immunology
|
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 .
|
-
- HY-109178
-
ATI-50002; ATI-502
|
JAK
|
Others
Inflammation/Immunology
|
Ifidancitinib (ATI-50002) is an orally available, potent and selective inhibitor of JAK kinase 1/3 that disrupts γc cytokine signaling. Ifidancitinib is used in the research of allergy, asthma, and autoimmune diseases .
|
-
- HY-18200A
-
E5555 hydrochloride; ER-172594-00 hydrochloride
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
|
-
- HY-124727
-
|
JAK
Apoptosis
|
Cancer
|
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
|
-
- HY-132849
-
TD-0903
|
JAK
|
Infection
Inflammation/Immunology
|
Nezulcitinib (TD-0903) is an inhaled and lung-selective pan-Janus kinase (JAK) inhibitor. Nezulcitinib can be used for the research of COVID-19 associated acute lung injury and impaired oxygenation .
|
-
- 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-W727879
-
ABT-494-15N,d2
|
Isotope-Labeled Compounds
|
Others
|
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
|
-
- HY-169984S
-
|
Isotope-Labeled Compounds
STAT
JAK
|
Inflammation/Immunology
|
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-145588A
-
INCB54707 phosphate
|
JAK
|
Inflammation/Immunology
|
Povorcitinib (INCB54707) phosphate is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib phosphate can be used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) (information extracted from patent WO2021076124A1).
|
-
- HY-145015
-
HM43239
|
FLT3
Apoptosis
|
Cancer
|
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-145015A
-
HM43239 hydrate
|
FLT3
Apoptosis
|
Cancer
|
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-102084
-
|
Interleukin Related
|
Inflammation/Immunology
|
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130 .
|
-
- 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-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-W740378
-
AFN-941
|
EGFR
JAK
|
Others
|
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
|
-
- HY-132193
-
|
RET
|
Cancer
|
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects .
|
-
- HY-50867
-
CEP-701; KT-5555
|
JAK
FLT3
Trk Receptor
Apoptosis
STAT
|
Cancer
|
Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
|
-
- 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 Lipopolysaccharides (HY-D1056)‑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) .
|
-
- 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-112809
-
|
Syk
Src
LRRK2
GSK-3
JAK
VEGFR
Aurora Kinase
|
Inflammation/Immunology
|
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin .
|
-
- HY-131968
-
|
JAK
Cytochrome P450
|
Inflammation/Immunology
|
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 .
|
-
- HY-149007
-
|
STAT
Apoptosis
|
Cancer
|
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers .
|
-
- 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-120214
-
|
Syk
RET
|
Inflammation/Immunology
|
TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases .
|
-
- 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 HER2, HER3, and downstream effectors .
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15315S1
-
|
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
-
- HY-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[1].
|
-
-
- 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[1].
|
-
-
- HY-W727879
-
|
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
|
-
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- HY-131968
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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-18300S
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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-50856S2
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Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .
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- HY-10409S
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Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research .
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- HY-15315S
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Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
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- HY-169984S
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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-U00318
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Alkynes
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JAK-IN-11 is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment . JAK-IN-11 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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