Deucravacitinib (hydrochloride)
Based on 35 publication(s) in Google Scholar
Deucravacitinib (BMS-986165) hydrochloride is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib hydrochloride blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib hydrochloride can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.
For research use only. We do not sell to patients.
- CAS No.: 1609392-28-0
- Formula: C20H20D3ClN8O3
- Molecular Weight:461.92
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Deucravacitinib (hydrochloride)
More- Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
- Nat Commun. 2025 Jul 29;16(1):6972. [Abstract]
- J Adv Res. 2026 Apr 24:S2090-1232(26)00358-9. [Abstract]
- Nat Chem Biol. 2022 Dec;18(12):1388-1398. [Abstract]
- Cell Rep Med. 2025 Feb 18;6(2):101970. [Abstract]
- Cell Death Differ. 2021 Feb;28(2):748-763. [Abstract]
- Clin Cancer Res. 2023 Apr 14;29(8):1592-1604. [Abstract]
- J Invest Dermatol. 2025 May 27:S0022-202X(25)00531-7. [Abstract]
- J Invest Dermatol. 2025 Apr 8:S0022-202X(25)00393-8. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Int J Mol Sci. 2023 May 25;24(11):9243. [Abstract]
- Int J Mol Sci. 2022 May 1;23(9):5040. [Abstract]
- Inflamm Bowel Dis. 2021 Oct 18;27(10):1674-1683. [Abstract]
- Arthritis Res Ther. 2021 Apr 19;23(1):120. [Abstract]
- iScience. 2024 Dec 10;28(1):111563. [Abstract]
- iScience. 2021 May 3;24(6):102498. [Abstract]
- J Biol Chem. 2022 May;298(5):101938. [Abstract]
- J Biotechnol. 2025 Mar:399:9-18. [Abstract]
- Med Microbiol Immunol. 2025 Nov 14;214(1):50. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Anticancer Drugs. 2025 Apr 1;36(4):280-289. [Abstract]
- Iran J Immunol. 2024 Sep 25;21(3). [Abstract]
- bioRxiv. 2026 May 29.
- Res Sq. 2026 Jan 6.
- bioRxiv. 2025 Oct 15.
- bioRxiv. 2025 Aug 16.
- Patent. US20250235450A1.
- medRxiv. 2025 Mar 01.
- Immune Sys. 2024;0:1–13
- bioRxiv. 2024 Jun 6:2024.06.04.595773. [Abstract]
- bioRxiv. 2024 May 9:2024.03.20.585925. [Abstract]
- bioRxiv. 2023 Jul 1.
- Patent. US20230147873A1.
- Patent. US20220339151A1.
- Patent. US20200345731A1.
Customer Validation & Images
-
IHC
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
-
WB
-
WB
Biological Activity
Deucravacitinib hydrochloride potently inhibits TYK2-dependent IFNα-induced STAT5 phosphorylation in human CD3+ T cells, with an IC50 of 2 nM[2].
Deucravacitinib hydrochloride potently inhibits TYK2-dependent IL-23-induced STAT3 phosphorylation in human CD161+ CD3+ T cells, with an IC50 of 9 nM[2].
Deucravacitinib hydrochloride potently inhibits TYK2-dependent IFNα-induced STAT5 phosphorylation in human whole blood with an IC50 of 13 nM, while exhibiting high functional selectivity for signaling pathways dependent on JAK2, JAK1 and JAK3[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Deucravacitinib (50 mg/kg; p.o.; twice daily) hydrochloride almost completely inhibits body weight loss and significantly reduces histological damage in a mouse model of anti-CD40-induced colitis[2].
Deucravacitinib (30 mg/kg; p.o.; once daily; for 3 consecutive months) hydrochloride is well tolerated in a mouse lupus model and exerts significant efficacy in preventing nephritis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (PK studies; IL-23-driven acanthosis psoriasis model)[2]
-
Dosage:7.5 mg/kg; 15 mg/kg; 30 mg/kg
-
Administration:p.o.; twice daily; 9 days
-
Result:Reduced ear thickness increase relative to vehicle, inhibited epidermal hyperplasia and inflammatory cellular infiltration, and dose-dependently reduced relative gene expression of IL-17a, IL-21, IL-23a, IL-23R, IL-12 (p35), and IL-12 (p40) in skin biopsies at 7.5 mg/kg twice daily.
Maintained drug levels at or above mouse whole blood IC50 (100 nM) for 19 hours at 7.5 mg/kg twice daily.
Achieved ear thickness inhibition equivalent to the anti-IL-23 adnectin positive control, reduced epidermal hyperplasia and inflammatory cellular infiltration, showed greater reduction of cytokine gene expression than the 7.5 mg/kg dose, and maintained drug levels at or above mouse whole blood IC50 for 21 hours at 15 mg/kg twice daily.
Provided greater ear thickness protection than the anti-IL-23 adnectin, more effectively inhibited epidermal hyperplasia and inflammatory cellular infiltration than the positive control, showed the greatest reduction of cytokine gene expression across all doses, and maintained drug levels at or above mouse whole blood IC50 for 24 hours at 30 mg/kg twice daily.
-
Animal Model:NZB/W (spontaneous lupus-prone nephritis model; treated for three months)[2]
-
Dosage:30 mg/kg
-
Administration:p.o.; once daily; three months
-
Result:Was well-tolerated, highly efficacious in protecting against nephritis, inhibited type I IFN-dependent gene expression in whole blood and kidneys, and was at least as effective as a blocking anti-IFNαR antibody control; efficacy correlated with coverage of the whole blood IC50 over dosing intervals.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
-
CAS No. 1609392-28-0
-
Molecular Weight 461.92
-
Formula C20H20D3ClN8O3
-
SMILES
COC1=C(C2=NN(C)C=N2)C=CC=C1NC3=C(N=NC(NC(C4CC4)=O)=C3)C(NC([2H])([2H])[2H])=O.Cl
-
Synonyms
BMS-986165 (hydrochloride)
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (35)
-
Journal Impact Factor
-
Most Recent
-
Ann Rheum Dis
Augmentation of immunothrombosis as a key mechanism underlying JAK inhibition associated hypercoagulability in rheumatoid arthritis. [Abstract]2025 Sep 25:S0003-4967(25)04383-3. PMID: 41006174 -
Nat Commun
Autocrine interferon poisoning mediates ADAR1-dependent synthetic lethality in BRCA1/2-mutant cancers. [Abstract]2025 Jul 29;16(1):6972. PMID: 40730818 -
J Adv Res
Long noncoding RNA AFAP1-AS1 aggravates immunotherapy resistance in NSCLC by enhancing JAK2 and TYK2 translation. [Abstract]2026 Apr 24:S2090-1232(26)00358-9. PMID: 42035912 -
Nat Chem Biol
2022 Dec;18(12):1388-1398. PMID: 36097295
Deucravacitinib (hydrochloride) purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2022 Dec;18(12):1388-1398. [Abstract]
Western blots measuring effects of VVD-118313 (5a) and BMS-986165 (BMS) (2 µM, 2 h) on JAK1 phosphorylation (pJAK1).
-
Cell Rep Med
2025 Feb 18;6(2):101970. PMID: 39938523 -
Cell Death Differ
2021 Feb;28(2):748-763. PMID: 32929218
Deucravacitinib (hydrochloride) purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Feb;28(2):748-763. [Abstract]
BMS-986165 (0.02-1 μM; 18 h).Cells are treated with the allosteric TYK2 inhibitor BMS-986165 (TYK2 Inh.). BMS-986165 dose-dependently inhibits upregulation of CASP5 in response to LPS in U937 macrophages.
-
Clin Cancer Res
MEK Inhibition Synergizes with TYK2 Inhibitors in NF1-Associated Malignant Peripheral Nerve Sheath Tumors. [Abstract]2023 Apr 14;29(8):1592-1604. PMID: 36799629
Deucravacitinib (hydrochloride) purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Apr 14;29(8):1592-1604. [Abstract]
Deucravacitinib (5-80 μM; 0-72 h). The specific TYK2 inhibitor deucravacitinib (BMS-986165) decreases MPNST cell proliferation at lower doses.
Deucravacitinib (hydrochloride) purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2023 Apr 14;29(8):1592-1604. [Abstract]
The combination of drugs inhibiting TYK2 and MEK block MPNST tumor growth in mice. Mice with JW23.3 MPNST xenograft tumors were treated daily with 30 mg/kg deucravacitinib (Deucra, BMS-986165), the combination of drugs, or vehicle control for 3 weeks or until tumors reached the maximum allowed volume.
-
J Invest Dermatol
Pharmacological Characterization of Zasocitinib (TAK-279): An Oral, Highly Selective, and Potent Allosteric TYK2 Inhibitor. [Abstract]2025 May 27:S0022-202X(25)00531-7. PMID: 40441292 -
J Invest Dermatol
2025 Apr 8:S0022-202X(25)00393-8. PMID: 40210114
Deucravacitinib (hydrochloride) purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2025 Apr 8:S0022-202X(25)00393-8. [Abstract]
BMS-986165 (10 mg/kg; Oral). Representative images of histopathology images taken from each experimental group.
-
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Int J Mol Sci
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes. [Abstract]2023 May 25;24(11):9243. PMID: 37298195 -
Int J Mol Sci
In Vitro Assays to Identify Metabolism-Disrupting Chemicals with Diabetogenic Activity in a Human Pancreatic β-Cell Model. [Abstract]2022 May 1;23(9):5040. PMID: 35563431 -
Inflamm Bowel Dis
2021 Oct 18;27(10):1674-1683. PMID: 33295611 -
Arthritis Res Ther
Mitochondrial protein CMPK2 regulates IFN alpha-enhanced foam cell formation, potentially contributing to premature atherosclerosis in SLE. [Abstract]2021 Apr 19;23(1):120. PMID: 33874983 -
iScience
2024 Dec 10;28(1):111563. PMID: 39868044 -
iScience
Mitochondrial CMPK2 mediates immunomodulatory and antiviral activities through IFN-dependent and IFN-independent pathways. [Abstract]2021 May 3;24(6):102498. PMID: 34142025 -
J Biol Chem
Mitogen-activated protein kinase phosphatase-1 controls PD-L1 expression by regulating type I interferon during systemic Escherichia coli infection. [Abstract]2022 May;298(5):101938. PMID: 35429501 -
J Biotechnol
2025 Mar:399:9-18. PMID: 39824361 -
Med Microbiol Immunol
Furamidine enhances IL-23-mediated autophagic response through IL-23R-TYK2-STAT3-dependent regulation of intracellular Ca²⁺ level to facilitate mycobacterial clearance in human macrophages. [Abstract]2025 Nov 14;214(1):50. PMID: 41236630 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Anticancer Drugs
Dual inhibition of TYK2 and PD-L1 boosts immune response in triple negative breast cancer. [Abstract]2025 Apr 1;36(4):280-289. PMID: 39774369 -
Iran J Immunol
2024 Sep 25;21(3). PMID: 39319693 -
-
-
-
-
-
-
-
bioRxiv
2024 Jun 6:2024.06.04.595773. PMID: 38895380 -
bioRxiv
Pharmacological inhibition of tyrosine protein-kinase 2 reduces islet inflammation and delays type 1 diabetes onset in mice. [Abstract]2024 May 9:2024.03.20.585925. PMID: 38766166 -
-
-
-
Purity & Documentation
References
[1]. Armstrong AW, et al. Deucravacitinib versus placebo and apremilast in moderate to severe plaque psoriasis: Efficacy and safety results from the 52-week, randomized, double-blinded, placebo-controlled phase 3 POETYK PSO-1 trial. J Am Acad Dermatol. 2023;88(1):29-39. [Content Brief]
[2]. Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019;62(20):8973-8995. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Deucravacitinib (hydrochloride) Related Classifications
HY-117287A Related Classifications
Powered by Bioz