Deucravacitinib (BMS-986165)

Catalog No.S8879 Batch:S887902

Technical Data

Formula	C₂₀H₁₉D₃N₈O₃
Molecular Weight	425.46	CAS No.	1609392-27-9
Solubility (25°C)*	In vitro	DMSO	30 mg/mL (70.51 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.

Targets

Tyk2 ^[1]
(Cell-free assay)

0.02 nM

In vitro

BMS-986165 is highly differentiated from all other reported JAK/TYK2 inhibitors due to its ability to achieve an unprecedented level of selectivity for TYK2, especially over JAK1, JAK2, and JAK3.^[1]

In vivo

BMS-986165 has been identified as a highly potent and selective allosteric TYK2 inhibitor having excellent PK properties across species with minimal profiling liabilities and is orally efficacious with dose-dependent activity in a murine disease model of psoriasis. Significant activity has also been observed with 11 in other murine autoimmune disease models of colitis and lupus.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines CD3+ T-cells, CD161+ CD3+ T-cells, TF-1 cells, mononuclear cells, platelets Concentrations 0 - 10 μM Incubation Time -- Method BMS-986165 is evaluated in both binding and human cellular assays to determine selectivity within the JAK family and across the kinome. Mean values are determined from at least three separate experiments unless otherwise noted. Measuring STAT5 phosphorylation in CD3+ T-cells as end point. Measuring STAT3 phosphorylation in CD161+ CD3+ T-cells. Measuring STAT5A phosphorylation in TF-1 cells (n = 2). Measuring STAT6 phosphorylation in mononuclear cells (n = 2). Measuring STAT5 phosphorylation in platelets. Measuring STAT3 phosphorylation in CD3+ T-cells.
Animal Study:^{^[1]}	Animal Models 6−8-week-old C57BL/6 female mice Dosages 7.5 mg/kg, 15 mg/kg, and 30 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

Cell lines
CD3+ T-cells, CD161+ CD3+ T-cells, TF-1 cells, mononuclear cells, platelets
Concentrations
0 - 10 μM
Incubation Time
--
Method
BMS-986165 is evaluated in both binding and human cellular assays to determine selectivity within the JAK family and across the kinome. Mean values are determined from at least three separate experiments unless otherwise noted. Measuring STAT5 phosphorylation in CD3+ T-cells as end point. Measuring STAT3 phosphorylation in CD161+ CD3+ T-cells. Measuring STAT5A phosphorylation in TF-1 cells (n = 2). Measuring STAT6 phosphorylation in mononuclear cells (n = 2). Measuring STAT5 phosphorylation in platelets. Measuring STAT3 phosphorylation in CD3+ T-cells.

Animal Study:^{^[1]}

Animal Models
6−8-week-old C57BL/6 female mice
Dosages
7.5 mg/kg, 15 mg/kg, and 30 mg/kg
Administration
Oral gavage

References

[1] Stephen T Wrobleski, et al. J Med Chem. 2019 Oct 24;62(20):8973-8995.

Selleck's Deucravacitinib (BMS-986165) has been cited by 6 publications

Type 1 interferons and Foxo1 down-regulation play a key role in age-related T-cell exhaustion in mice [ Nat Commun, 2024, 15(1):1718]	PubMed: 38409097
TYK2 signaling promotes the development of autoreactive CD8+ cytotoxic T lymphocytes and type 1 diabetes [ Nat Commun, 2024, 15(1):1337]	PubMed: 38351043
Type I interferon signaling induces melanoma cell-intrinsic PD-1 and its inhibition antagonizes immune checkpoint blockade [ Nat Commun, 2024, 15(1):7165]	PubMed: 39187481
A genome-scale screen identifies sulfated glycosaminoglycans as pivotal in epithelial cell damage by Candida albicans [ bioRxiv, 2024, 2024.05.23.595417]	PubMed: 38826446
Deucravacitinib, a tyrosine kinase 2 pseudokinase inhibitor, protects human EndoC-βH1 β-cells against proinflammatory insults [ Front Immunol, 2023, 10.3389/fimmu.2023.1263926]	PubMed: 37854597
Evolutionarily conserved regulators of tau identify targets for new therapies [ Neuron, 2022, S0896-6273(22)01085-6]	PubMed: 36610398

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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