2. Autophagy Apoptosis
  3. ULK Autophagy Apoptosis
  4. SBI-0206965

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2.

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

SBI-0206965 Chemical Structure

SBI-0206965 Chemical Structure

CAS No. : 1884220-36-3

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10 mM * 1 mL in DMSO
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10 mg USD 132 In-stock
50 mg USD 385 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

SBI-0206965 Related Antibodies

Top Publications Citing Use of Products

    SBI-0206965 purchased from MedChemExpress. Usage Cited in: BioMedicine. 2018 Aug;34:85-93.  [Abstract]

    A498 and ACHN cells are cultured in starvation medium (EBSS) with SBI-0206965 (0 μM, 5 μM, 10 μM, and 20 μM) for 24 h. Phosphorylation of Ser108 of the AMPK β1 subunit, cleavage of PARP and Caspase 8, and levels of LC3B and p62 are measured by western blot analysis.

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    ULK1 ULK2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2[1].

    IC50 & Target[1]

    ULK1

    108 nM (IC50)

    ULK2

    711 nM (IC50)

    In Vitro

    SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation[1].
    SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis[1].

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

    SBI-0206965 Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: A498 and ACHN cells (starvation medium (EBSS) treatment)
    Concentration: 5, 10 ,20 μM
    Incubation Time: 24 hours
    Result: Induced significant levels of apoptosis.

    Western Blot Analysis[1]

    Cell Line: A498 and ACHN cells (EBSS treatment)
    Concentration: 5, 10, 20 μM
    Incubation Time: 24 hours
    Result: Attenuated the phosphorylation of Ser108 of the AMPK β1 subunit and increased the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluated by analysis of LC3B and p62.
    In Vivo

    SBI-0206965 (50 mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours[1].

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

    Animal Model: Six-week-old male BALB/c nude mice (A498 xenograft tumours)[1]
    Dosage: 50 mg/kg
    Administration: Intraperitoneal injection; once every three days for 37 days
    Result: Significantly suppressed tumour growth.
    Molecular Weight

    489.32

    Formula

    C21H21BrN4O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CNC(C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (204.37 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0437 mL 10.2183 mL 20.4365 mL
    5 mM 0.4087 mL 2.0437 mL 4.0873 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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

    Concentration (start)

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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: ≥ 2.5 mg/mL (5.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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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:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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

    Purity: 99.39%

    COA (252 KB) LCMS (95 KB) Elemental Analysis Report (111 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0437 mL 10.2183 mL 20.4365 mL 51.0913 mL
    5 mM 0.4087 mL 2.0437 mL 4.0873 mL 10.2183 mL
    10 mM 0.2044 mL 1.0218 mL 2.0437 mL 5.1091 mL
    15 mM 0.1362 mL 0.6812 mL 1.3624 mL 3.4061 mL
    20 mM 0.1022 mL 0.5109 mL 1.0218 mL 2.5546 mL
    25 mM 0.0817 mL 0.4087 mL 0.8175 mL 2.0437 mL
    30 mM 0.0681 mL 0.3406 mL 0.6812 mL 1.7030 mL
    40 mM 0.0511 mL 0.2555 mL 0.5109 mL 1.2773 mL
    50 mM 0.0409 mL 0.2044 mL 0.4087 mL 1.0218 mL
    60 mM 0.0341 mL 0.1703 mL 0.3406 mL 0.8515 mL
    80 mM 0.0255 mL 0.1277 mL 0.2555 mL 0.6386 mL
    100 mM 0.0204 mL 0.1022 mL 0.2044 mL 0.5109 mL
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    SBI-0206965 Related Classifications

    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.

    Keywords:

    SBI-02069651884220-36-3SBI0206965SBI 0206965ULKAutophagyApoptosisUnc-51 like kinaseInhibitorinhibitorinhibit

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