Deucravacitinib | Allosteric TYK2 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $100.00 | ||
| 25 mg | $375.00 |
Deucravacitinib (1609392-27-9) is very potent and selective allosteric inhibitor of tyrosine kinase 2 (TYK2). It binds to and is selective for the TYK2 pseudokinase domain (JH2, IC50 = 0.2 nM), with no activity against canonical JH1 domain of TYK2, JAK1,2, or 3.1 It is 5-fold less active against the JAK1 JH2 domain (IC50 = 1 nM). Deucravacitinib blocked signaling and functional responses in human TH17, TH1, B cells, and myeloid cells and displayed robust efficacy in vitro and in vivo in autoimmune disease animal models.2
References/Citations:
- Wrobleski et al. (2019), Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165; J. Med. Chem. 62 8973
- Burke et al. (2019), Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain; Sci. Transl. Med. 11 eaaw1736
NMR (Conforms)
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Product Data Sheet:
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Deucravacitinib (1609392-27-9) is very potent and selective allosteric inhibitor of tyrosine kinase 2 (TYK2). It binds to and is selective for the TYK2 pseudokinase domain (JH2, IC50 = 0.2 nM), with no activity against canonical JH1 domain of TYK2, JAK1,2, or 3.1 It is 5-fold less active against the JAK1 JH2 domain (IC50 = 1 nM). Deucravacitinib blocked signaling and functional responses in human TH17, TH1, B cells, and myeloid cells and displayed robust efficacy in vitro and in vivo in autoimmune disease animal models.2
References/Citations:
- Wrobleski et al. (2019), Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165; J. Med. Chem. 62 8973
- Burke et al. (2019), Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain; Sci. Transl. Med. 11 eaaw1736
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