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Chemical Structure : JAK3 inhibitor RB1
Catalog No.: PC-22202Not For Human Use, Lab Use Only.
JAK3 inhibitor RB1 is a potent, selective and irreversible JAK3 inhibitor with IC50 of 40 nM, without inhibiting JAK1, JAK2 or TYK2 (IC50>5000 nM).
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JAK3 inhibitor RB1 is a potent, selective and irreversible JAK3 inhibitor with IC50 of 40 nM, without inhibiting JAK1, JAK2 or TYK2 (IC50>5000 nM).
RB1 exhibits excellent selectivity over TEC family (BMX, BTK, ITK, TXK, and TEC), the ErbB family (EGFR, ERBB4, and ERBB2), and BLK.
RB1 inhibits the phosphorylation of STAT5 elicited by IL-2 at IC50 values of 105 nM in human peripheral blood mononuclear cells (PBMCs), shows 400-fold selectivity over the IL-2 stimulated pathway.
RB1 covalently modify JAK3 Cys909 in an apparently irreversible manner.
RB1 (10 mg/kg, 30 mg/kg or 100 mg/kg) is efficacious in treating a collagen-induced arthritis model, inhibits the JAK-STAT pathway.
| M.Wt | 271.32 | |
| Formula | C14H17N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Pei H, et al. Sci Rep. 2018 Mar 27;8(1):5273.
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