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TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $99 | 6-8 weeks |
Description | TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2. |
Targets&IC50 | GSK-3β:3 nM, JAK3:8 nM, JAK1:1.017 μM, PKCα:13 nM, JAK2:2.55 μM, PKCθ:68 nM |
In vitro | TCS 21311 displays moderate activity in this cellular assay (IC50=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity. TCS 21311 shows IC50 values of 1.017, 2.550, and 8.055 μM for JAK1, JAK2, and TYK2, respectively?in an enzymatic Jak assay [1]. |
Alias | NIBR3049 |
Molecular Weight | 526.51 |
Formula | C27H25F3N4O4 |
Cas No. | 1260181-14-3 |
Smiles | CC(C)(O)C(=O)N1CCN(CC1)c1ccc(c(c1)C1=C(C(=O)NC1=O)c1c[nH]c2ccccc12)C(F)(F)F |
Relative Density. | 1.436 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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