1. Apoptosis
  2. RIP kinase
  3. HS-1371

HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM.

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

CAS No. : 2158197-70-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    HS-1371 purchased from MedChemExpress. Usage Cited in: Nature. 2023 Mar;615(7950):158-167.  [Abstract]

    Cell viability assessment in Tbk1-null B16 cells pre-treated with RIPK3 inhibitor (HS-1371, 2 μM) or MLKL inhibitor (GW806742X, 5 μM) and the pan-caspase inhibitor Q-VD-Oph (20 μM) +/− TNFα/IFNγ for 9 days (n=6, 2 independent experiments: 2-way ANOVA, Dunnett’s multiple comparisons test).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM[1].

    IC50 & Target

    IC50: 20.8 nM (RIP3)[1]

    In Vitro

    HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner. HS-1371 has an inhibitory effect on RIP3 kinase activity in various cell lines[1].

    HS-1371 (0.1, 1, 5, 10, 20 μM, 9 h) can block RIP3 S227 phosphorylation[1].

    HS-1371 (0.1, 1, 5, 10 μM, 24 h) rescues cells from RIP3-dependent necroptotic cell death but not apoptotic cell death[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[1]

    Cell Line: HT-29 cells 
    Concentration: 0.1, 1, 5, 10, 20 μM
    Incubation Time: 9 hours
    Result: Showed an inhibitory effect on S227 auto-phosphorylation of RIP3[1].
    Molecular Weight

    384.47

    Formula

    C24H24N4O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1=CC=C(OC2=CC=NC3=CC(C4=CN(C5CCNCC5)N=C4)=CC=C23)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 16.67 mg/mL (43.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6010 mL 13.0049 mL 26.0098 mL
    5 mM 0.5202 mL 2.6010 mL 5.2020 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 1.67 mg/mL (4.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.67 mg/mL (4.34 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    %
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    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6010 mL 13.0049 mL 26.0098 mL 65.0246 mL
    5 mM 0.5202 mL 2.6010 mL 5.2020 mL 13.0049 mL
    10 mM 0.2601 mL 1.3005 mL 2.6010 mL 6.5025 mL
    15 mM 0.1734 mL 0.8670 mL 1.7340 mL 4.3350 mL
    20 mM 0.1300 mL 0.6502 mL 1.3005 mL 3.2512 mL
    25 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6010 mL
    30 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1675 mL
    40 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6256 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    HS-1371
    Cat. No.:
    HY-114349
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