Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 64.00 | |
5 mg | In stock | $ 155.00 | |
10 mg | In stock | $ 289.00 | |
25 mg | In stock | $ 455.00 | |
50 mg | In stock | $ 672.00 | |
100 mg | In stock | $ 956.00 | |
200 mg | In stock | $ 1,290.00 | |
500 mg | In stock | $ 1,920.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 169.00 |
Description | Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. |
Targets&IC50 | JAK1 JH2:1 nM, Tyk2 JH2:0.2 nM |
In vitro | BMS-986165 maintains excellent potency in human and mouse whole blood (IC50s=13 and 100 nM, respectively). Which shows no significant hERG inhibition in the flux assay (IC50>80 μM).BMS-986165 is differentiated from previous JAK inhibitors due its unique ability to selectively bind to the pseudokinase (JH2) domain of TYK2 and inhibit its function through an allosteric mechanism[1]. |
In vivo | BMS-986165 as a high affinity JH2 ligand and potent allosteric inhibitor of TYK2. In addition to unprecedented JAK isoform and kinome selectivity, BMS-986165 shows excellent pharmacokinetic properties with minimal profiling liabilities and is efficacious in several murine models of autoimmune disease. On the basis of these findings, BMS-986165 appears differentiated from all other reported JAK inhibitors and has been advanced as the first pseudokinase-directed therapeutic in clinical development as an oral treatment for autoimmune diseases[1]. |
Synonyms | BMS-986165 |
Molecular Weight | 425.46 |
Formula | C20H19D3N8O3 |
CAS No. | 1609392-27-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32.5mg/ml (76.39 Mm), sonification is recommended.
You can also refer to dose conversion for different animals. More
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Deucravacitinib 1609392-27-9 Angiogenesis Chromatin/Epigenetic Immunology/Inflammation JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK IFNAR Interleukin Janus kinase inhibit Interleukin Related Interferon-alpha/beta receptor Interferon-α/β receptor Inhibitor BMS 986165 BMS986165 BMS-986165 inhibitor