Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約10-14 週間 | ¥ 555,500 |
50 mg | 約10-14 週間 | ¥ 730,000 |
100 mg | 約10-14 週間 | ¥ 987,000 |
ターゲット&IC50 | TYK2:72 nM, IKKβ:9 nM |
In vitro | BMS-066 demonstrates significant inhibition of IKKβ-catalyzed phosphorylation in vitro, with a potent IC50 of 9 nM, exhibiting over 500-fold selectivity towards IKKβ compared to IKKα. In assays with six kinases that were more than 75% inhibited at 10 μM, BMS-066 displayed over 30-fold selectivity over the next most susceptible kinase (Brk), indicating its specificity. Additionally, BMS-066 showed IC50 values of 72 and 1020 nM in Tyk2 pseudokinase domain probe displacement and IL-23-stimulated reporter assays respectively. A broader selectivity assessment against 155 kinases at 10 μM revealed that only six were inhibited more than 75%, confirming BMS-066's greater than 400-fold selectivity for IKKβ over 95% of the kinases tested. BMS-066 also effectively inhibits LPS-stimulated cytokine production in human peripheral blood mononuclear cells (PBMCs) at both protein and mRNA levels, with similar IC50 values around 200 nM, and it inhibits IKKβ-mediated phosphorylation of IkBα in LPS-stimulated cells with a comparable efficacy. |
分子量 | 379.42 |
分子式 | C19H21N7O2 |
CAS No. | 914946-88-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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BMS-066 914946-88-6 NF-Κb Tyrosine Kinase/Adaptors Tyrosine Kinases IκB/IKK BMS 066 BMS066 Inhibitor inhibitor inhibit