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

SBI-0206965 

Cat. No.: HY-16966 Purity: 98.76%
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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 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.

    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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    • 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 .

    IC50 & Target

    IC50: 108 nM (ULK1 kinase), 711 nM (ULK2 kinase)[2]

    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].

    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].

    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.

    1884220-36-3

    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)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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 provided by MCE.
    References

    Purity: 98.76%

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    Product name:
    SBI-0206965
    Cat. No.:
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