JAK Inhibitor

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).

JAK/HDAC-IN-3 (13a) is a dual JAK and HDAC inhibitor, with IC₅₀ values of 25.36 nM, 0.2 μM and 0.43 μM for JAK2, HDAC and HDAC1, respectively.

JAK2-IN-21 is a Janus kinase 2 (JAK2) inhibitor with an IC₅₀ of 12.25 nM. JAK2-IN-21 inhibits the JAK2/STAT3/STAT5 tumor-promoting signaling pathway and reduces JAK2 protein expression. JAK2-IN-21 exhibits selective cytotoxicity against HPV-positive cancer cells and induces cancer cell apoptosis. JAK2-IN-21 can be used in the research of HPV-positive cervical cancer.

JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.

Jak3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Jak3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

JAK2-IN-12 (compound 23) is a JAK2 inhibitor with a pIC₅₀ of 8.2. JAK2-IN-12 can be used for study of myelofibrosi.

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.

PI3K/Akt/mTOR-IN-7 is an AKT/mTOR and JAK2/STAT3 inhibitor. PI3K/Akt/mTOR-IN-7 restores p-Akt, p-mTOR, and p-STAT3 expression, reduces pro-apoptotic Caspase-3 mRNA expression. PI3K/Akt/mTOR-IN-7 reduces intracellular ROS accumulation and inhibits NO production. PI3K/Akt/mTOR-IN-7 can be used for research on stroke, Alzheimer's disease and Parkinson's disease.

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).

JAK2-IN-23 is a highly selective JH2-binding JAK2 inhibitor, with an IC₅₀ ≤ 10 nM for binding to both wild-type and V617F-mutated JH2. JAK2-IN-23 can be used in studies of JAK2-related diseases, such as cancer.

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.

Radotinib-d₆ is deuterium labeled Radotinib (HY-15728). Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC₅₀ of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.

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.

STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.

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.

JAK3-IN-17 (Compound X15) is an orally active JAK3 inhibitor (IC₅₀: 14.56 nM). JAK3-IN-17 inhibits the production of IL-2 and IL-6 in a DNCB-induced mouse atopic dermatitis model and exhibits anti-inflammatory activity.

GDC-9918 (compund GDC-9918) is a Janus kinase inhibitor.

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)

JAK-IN-29 (compound 3) is a potent JAK inhibitor.

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective JAK1 inhibitor.