jak in 1

JAK-IN-1 shows improved selectivity for JAK3 over JAK1. JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.

DualCathepsinL/JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1/2/3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL/JAK-IN-1 is applicable in research on acute lung injury (ALI).

SYK/JAK-IN-1 is a dual SYK/JAK inhibitor with IC50 values of less than 5 nM for both SYK and JAK2.

JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.

JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

JAK2/STAT3-IN-1 is a GP130 inhibitor with anti-tumor effects and can be used to study inflammation, autoimmunity and cancer.

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 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).

JAK3-IN-1 is an orally active, selective and potent JAK3 inhibitor that can be used to study immune system diseases.

JAK1-IN-8, a specific inhibitor of Janus kinase 1 (JAK1, IC50<500 nM).

JAK-2/3-IN-1 is a highly effective inhibitor targeting both JAK-2 and JAK-3 isoforms, exhibiting remarkable potency with Ki values below 250 nM for both isoforms.

JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 [IC50 = 29 nM] and JAK1 (IC50 = 41 nM).

JAK1-IN-9 (compound 23a) is a potent, selective JAK1 inhibitor with an IC50 of 72 nM, exhibiting over 12-fold selectivity against other JAK family members [1].

HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4. This compound not only inhibits cell proliferation but also induces apoptosis in MDA-MB-231 cells and demonstrates in vivo anticancer efficacy [1].

JAK kinase-IN-1 (Example 1) is a potent inhibitor targeting the JAK family, including TYK2, JAK1, JAK2, and JAK3, with IC50 values of 4.2 nM, 32 nM, 27 nM, and 3473 nM, respectively [1].

JAK1/TYK2-IN-4 serves as a dual inhibitor targeting both JAK and TYK2, displaying IC50 values of 39 nM and 21 nM, respectively. It is also orally bioavailable [1].

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and demonstrating a 246-fold selectivity compared to other JAKs.

JAK1-IN-16 (compound 4l) acts as an inhibitor of JAK1/STAT3 and effectively downregulates the expression of TLR4 protein.

JAK1/STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1/STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1/STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1/JAK1 and p-STAT3/STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).

JAK1-IN-14 (Compound12a) is a potent and selective inhibitor of JAK1, effectively inhibiting JAK1 and JAK2 with IC50 values of 12.6 nM and 135 nM, respectively. It reduces liver fibrosis levels and is applicable for research related to liver fibrosis and inflammatory diseases.

JAK1/2-IN-1 is a potent inhibitor of JAK1 and JAK2, with IC50 values of 0.4 nM and 8.1 nM, respectively. Additionally, JAK1/2-IN-1 inhibits IL-4 and IL-13, with IC50 values of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).

PROTACJAK1 degrader 1 (compound 10c) is a potent and selective PROTAC JAK1 degrader with a DC50 of 214 nM. It also exhibits antitumor activity.

PROTAC JAK2 degrader-1 (Compound 10i) is a JAK2 PROTAC degrader with a DC50 of 27.35 nM against JAK2V617F. It facilitates the ubiquitination and degradation of JAK2. This compound also inhibits the phosphorylation of JAK2, STAT3, and STAT5, and is applicable in the study of myeloproliferative neoplasms.

JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 value of 0.15 nM, demonstrating significantly greater inhibitory potency for JAK1 compared to JAK2 and JAK3. It significantly reduces inflammation in ulcerative colitis (UC) mouse models induced by DSS and Crohn's disease (CD) rat models induced by DNBS. JAK1-IN-18 is applicable for research into autoimmune diseases (such as inflammatory bowel disease), viral infections (such as hepatitis B virus infection), and cancers (such as hematologic malignancies).