1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Immunology/Inflammation
  2. JAK
    Interleukin Related
    IFNAR
  3. BMS-986165

BMS-986165 

Cat. No.: HY-117287 Purity: 99.79%
Handling Instructions

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. BMS-986165 inhibits IL-12/23 and type I IFN pathways.

For research use only. We do not sell to patients.

BMS-986165 Chemical Structure

BMS-986165 Chemical Structure

CAS No. : 1609392-27-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE BMS-986165

    BMS-986165 purchased from MCE. Usage Cited in: Cell Death Differ. 2020 Sep 14.

    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. CASP4 is constitutively expressed and not further upregulated by LPS.

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    Description

    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. BMS-986165 inhibits IL-12/23 and type I IFN pathways[1][2].

    IC50 & Target

    Tyk2 JH2

    0.2 nM (IC50)

    JAK1 JH2

    1 nM (IC50)

    IL-12

     

    IL-23

     

    In Vitro

    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].
    BMS-986165 maintains excellent potency in human and mouse whole blood (IC50s=13 and 100 nM, respectively) and shows no significant hERG inhibition in the flux assay (IC50>80 μM)[1].

    Clinical Trial
    Molecular Weight

    425.46

    Formula

    C₂₀H₁₉D₃N₈O₃

    CAS No.

    1609392-27-9

    SMILES

    O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 37.5 mg/mL (88.14 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3504 mL 11.7520 mL 23.5040 mL
    5 mM 0.4701 mL 2.3504 mL 4.7008 mL
    10 mM 0.2350 mL 1.1752 mL 2.3504 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.79%

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    Keywords:

    BMS-986165BMS986165BMS 986165JAKInterleukin RelatedIFNARJanus kinaseILInterferon-α/β receptorInterferon-alpha/beta receptorInhibitorinhibitorinhibit

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    Product Name:
    BMS-986165
    Cat. No.:
    HY-117287
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