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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 |
|---|
| AG490
AG490 (Tyrphostin AG490) is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). |
| AZ 960
AZ 960 is a novel and specific inhibitor of the JAK2 kinase with a Ki of 0.45nM in vitro. |
| Momelotinib (CYT387)
Momelotinib (CYT387) is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively. |
| TG101348
TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM. |
| WP1130
Degrasyn (WP1130) is a small molecular deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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