RO495 is a potent inhibitor of non-receptor tyrosine-protein kinase 2 (TYK2 kinase)[1].
TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD)[1].
Momelotinib-3,3,5,5-d4 (CYT387-3,3,5,5-d4) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF)[1][2][3].
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[1].
Momelotinib-2,2,6,6-d6 (CYT387-2,2,6,6-d6) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.
Rovadicitinib hydrochloride is a JAK inhibitor with an IC50 value <20 nM. Rovadicitinib hydrochloride also exhibits anti-inflammatory activity[1][2].
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon[1].
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[1].
Deuruxolitinib (CTP-543), a deuterated Ruxolitinib, modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I)[1].
JAK-IN-34 (compound 11n) is a potent against of JAKs with IC50 values of 0.40, 0.83, 2.10, 1.95 nM target JAK1, JAK2, JAK3, TYK2, respectively. JAK-IN-34 reduces joint swelling with good safety[1].
Momelotinib-2,2,6,6-d4 (CYT387-2,2,6,6-d4) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally acitve and ATP-competitive JAK1/JAK2 inhibitor with IC50s of 11 nM and 18 nM, respectively[1][2].
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[1].
Tyk2-IN-8 (Compound 3) 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].
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable drug metabolism and pharmacokinetics profile[1].
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)[1].
(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[1].
Momelotinib-d2 (CYT387-d2) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally active and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
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.
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases[1]. 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.
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
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[1].
JAK3i is a selective, covalent JAK3 kinase inhibitor with IC50 of 0.43 nM, shows high selectivity (>3,000-fold) against the closely related kinase domains in JAK1, JAK2, or TYK2, displays 1,300-fold, 600-fold, and 50-fold over EGFR, ITK, and BTK respectively.
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[1][2].
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety[1].
Oclacitinib is a novel JAK inhibitor. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM).
ABBV-712 is a selective inhibitor of Tyrosine kinase 2 (TYK2), with IC50 of 0.195 μM, that play important role in autoimmune diseases[1].
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[1].
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)[1]