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SBI-0206965

SKU: orb1225827

Description

SBI-0206965 (SBI 0206965) is a potent and specific small molecule ULK1 kinase inhibitor with IC50 of 108 nM; displays 7-fold less potency for ULK2 (IC50=711 nM); inhibits Beclin1 Ser15 and Vps34 Ser249 phosphorylation to comparable extents in HEK-293T cells; suppresses autophagy induced by mTOR inhibition and prevents ULK1-dependent cell survival; greatly synergized with mTOR inhibitors to kill tumor cells.

Images & Validation

Key Properties

CAS Number1884220-36-3
MW489.3192
Purity>98% (HPLC)
FormulaC21H21BrN4O5
SMILESO=C(NC)C1=CC=CC=C1OC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Br
TargetULK
Solubility10 mM in DMSO

Bioactivity

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. Animal model: Six-week-old male BALB/c nude mice (A498 xenograft tumours). Dosage: 50 mg/kg. Administration: Intraperitoneal injection; once every three days for 37 days. Result: Significantly suppressed tumour growth.
In Vitro
SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation. 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. Apoptosis Analysis 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. 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SBI 0206965 | SBI0206965

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SBI-0206965 (orb1225827)

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200 mg
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2 mg
$ 80.00
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$ 160.00
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50 mg
$ 400.00
100 mg
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