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MedChemExpressModel SBI-0206965 -1884220-36-3

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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].
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SBI-0206965

MCE China:SBI-0206965

Brand:MedChemExpress (MCE)

Cat. No.HY-16966

CAS:1884220-36-3

Purity:99.92%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

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.

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].

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].

IC50 & Target:ULK1 108 nM (IC50) ULK2 711 nM (IC50)

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References:

[1]. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell RenalCarcinoma and the Antitumor Effects of SBI-0206965. EBioMedicine. 2018 Aug;34:85-93.  [Content Brief]

[2]. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-97.  [Content Brief]

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