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

SBI-0206965 

Cat. No.: HY-16966 Purity: 99.39%
COA Handling Instructions

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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 83 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 83 In-stock
Solid
5 mg USD 77 In-stock
10 mg USD 132 In-stock
50 mg USD 385 In-stock
100 mg USD 605 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 16 publication(s) in Google Scholar

Top Publications Citing Use of Products

    SBI-0206965 purchased from MCE. 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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    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

    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].

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

    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].

    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

    Appearance

    Solid

    Formula

    C21H21BrN4O5

    CAS No.
    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)

    *"≥" 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
    10 mM 0.2044 mL 1.0218 mL 2.0437 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: ≥ 2.5 mg/mL (5.11 mM); Clear solution

    • 2.

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

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.39%

    References
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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.

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    Product Name:
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    Cat. No.:
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