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Home > Inhibitors & Agonists > JAK/STAT Signaling > JAK

JAK

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Cat. No. Product Name Field of Application Chemical Structure
DC81771 YN11
YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer.
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DC81578 STING agonist-50
STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer.
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DC81482 S1PR1/S1PR5 agonist-1
S1PR1/S1PR5 agonist-1 (Compound 19) is an orally active S1PR1 and S1PR5 agonist with EC50 values of 40.0 and 22.9 nM, respectively. S1PR1/S1PR5 agonist-1 binds to key residues of S1PR1 to mediate agonistic activity. S1PR1/S1PR5 agonist-1 alleviates colitis pathological changes in DSS-induced mouse models and exerts minimal effects on mouse heart rate. S1PR1/S1PR5 agonist-1 can be used for the research of inflammatory bowel disease.
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DC81356 PROTAC EZH2 Degrader-19
PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer. (Pink: EZH2 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).
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DC81241 PARP1-IN-51
PARP1-IN-51 (P55 the second compound in the fifth row) is a PARP1 inhibitor. PARP1-IN-51 can be used for the research of cancer, such as breast cancer.
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DC81153 NIP 502
NIP 502 is a pyridazinone derivative with orally active anti-inflammation and anti-immunology effects. NIP 502 can be used for the research of asthma.
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DC80669 Fmoc-Asp(OtBu)-OH-15N
Fmoc-Asp(OtBu)-OH-15N is the 15N-labeled Fmoc-Asp(OtBu)-OH. Fmoc-Asp(OtBu)-OH (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate) is an aspartate derivative containing amine protecting group Fmoc. Fmoc-Asp(OtBu)-OH can be used for peptide synthesis.
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DC80557 DNMT-IN-6
DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma.
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DC80554 DNA-PK/HDAC6-IN-1
DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia.
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DC79854 Voderdeucitinib
Voderdeucitinib (Compoudn I) is a TYK2 inhibitor with an anti-inflammatory activity. Voderdeucitinib can be used for inflammatory and autoimmune disease research, such as rheumatoid arthritis (RA), multiple sclerosis and intestinal bowel disease (IBD).
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DC79847 Butyzamide
Butyzamide (GMP) is Butyzamide) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of platelets in mouse xenotransplantation assay.
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DC79236 WP-1034
WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research.
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DC79141 (Rac)-TUL01101
(Rac)-TUL01101 (Compound I) is a selective JAK kinase inhibitor. (Rac)-TUL01101 can be used in the research of various diseases such as rheumatoid arthritis, atopic dermatitis, and alopecia areata.
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DC78882 Quecitinib
Quecitinib (QY201) is an orally active JAK1/TYK2 dual inhibitor. Quecitinib is also a substrate of cytochrome P450 3A and is mainly metabolized to mono-oxide and glucuronidation products. Quecitinib has favorable pharmacokinetic properties as well as safety. Quecitinib can be used in the research of atopic dermatitis and other autoimmune diseases.
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DC78635 Modzatinib
Modzatinib (ITK kinase-IN-1) (compound I) is an inhibitor targeting ITK kinase (IC50=8 nM, Jurkat cells) and can be used to study inflammatory diseases. Modzatinib has an IC50 of 23 nM for JAK3 in hPBMC cells (based on IL-2/pSTAT5 levels), wihout inhibitory effect against JAK2.
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DC78549 Socrodeucitinib
Socrodeucitinib (Compound Example 58) is an orally active and selective tyrosine kinase 2 (TYK2) inhibitor with an IC50 value of 1.41 nM. Socrodeucitinib exerts anti-inflammatory activity by inhibiting TYK2-mediated cytokine signaling pathways and reducing the secretion of inflammatory factors. Socrodeucitinib is promising for research of autoimmune diseases such as psoriasis and inflammatory diseases.
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DC78512 DEL1187-126-28-16
DEL1187-126-28-16 is a JAK3 inhibitor with IC50s of 10 and 0.97 nM against JAK3 WT in 0 and 60 min. DEL1187-126-28-16 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-28-16 can be used for the study of immune-mediated diseases.
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DC78086 Soficitinib
Soficitinib (Compound 20) is a selective inhibitor targeting tyrosine kinase 2 (TYK2) and Janus kinase 2 (JAK2) with an IC50 values of 0.5 nM and 1.2 nM, respectively. Soficitinib is promising for research of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis) and inflammatory diseases.
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DC78022 DEL1187-126-5-80
DEL1187-126-5-80 is a JAK3 inhibitor with IC50s of 52 and 7.9 nM against JAK3 WT in 0 and 60 min. DEL1187-126-5-80 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-5-80 can be used for the study of immune-mediated diseases.
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DC8171 Decernotinib (VX-509,adelatinib) Featured
Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
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DC76727 Golidocitinib 1-hydroxy-2-naphthoate
Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).
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DC76726 (3R,4S)-Tofacitinib
(3R,4S)-Tofacitinib is a less active enantiomer of Tofacitinib and a first-in-class inhibitor of JAK3 with an IC50 of 1 nM. It is highly efficacious in treating rheumatoid arthritis (RA).
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DC76725 Milpecitinib
Milpecitinib (Compound 21a) is a potent, selective Janus tyrosine kinase (JAK) inhibitor with anti-inflammatory activity. Milpecitinib is promising for research of cancers and inflammatory disorders.
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DC76724 LNK01004
LNK01004 is a JAK inhibitor with strong inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50:<0.51 nM) and TYK2 (IC50: 1.0 nM) . LNK01004 can simultaneously inhibit multiple cytokine-induced p-STAT signaling pathways. LNK01004 can be used in the research of diseases such as atopic dermatitis.
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DC76723 lirucitinib
lirucitinib is a JAK inhibitor, and has antiinflammatory activity
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DC76722 JNN-5
JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157).
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DC76721 iBFAR2
iBFAR2, a BFAR inhibitor, restores the CD8+ TRM cell subset against solid tumors. iBFAR2 promotes JAK2-STAT1 association and STAT1 phosphorylation.
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DC73569 Lepzacitinib (ATI-1777) Featured
Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases.
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DC70233 Londamocitinib(AZD4604) Featured
AZD4604 (AZD-4604) is a potent, selective Janus-associated kinase 1 (JAK1) inhibitor with anti-inflammatory effect.
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DC47030 Ilunocitinib Featured
Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).
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