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Delgocitinib, also known as LEO-124249 and JTE052, is a potent and selective JAK inhibitor with IC50 values of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α with IC50 values of 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively. Delgocitinib also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50=8.9±3.6 nM). JTE-052 reduces skin inflammation and ameliorates chronic dermatitis in rodent models. JTE-052 regulates contact hypersensitivity by downmodulating T cell activation and differentiation.
| Molecular Weight | 310.35 |
| Formula | C16H18N6O |
| CAS Number | 1263774-59-9 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related JAK Products |
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| iJak-381
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. |
| Ritlecitinib (malonate)
Ritlecitinib (PF-06651600) malonate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. |
| Deuruxolitinib
Deuruxolitinib is a deuterated Ruxolitinib (INCB18424), which modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research of hair loss disorders. |
| A-005
A-005 is a potentially first-in-class, brain-penetrating TYK2 allosteric inhibitor for studies related to neuroinflammatory and neurodegenerative diseases. |
| Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9)
Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide corresponding to amino acids 475 to 491 of mouse JAK2. |
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