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SBI-0206965

Cat. No. M6086
SBI-0206965 Structure
Synonym:

SBI 0206965; SBI0206965

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 120 In stock
5mg USD 100 In stock
10mg USD 150 In stock
50mg USD 450 In stock
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Quality Control
Biological Activity

SBI-0206965 has very high selectivity, only inhibits 10 out of 456 kinases >95% when tested at 10 μM. SBI-0206965 suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival It can suppress autophagy induced by mTOR inhibition, prevent ULK1-dependent cell survival following nutrient deprivation. It greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic.

Protocol
Cell Experiment
Cell lines HEK-293T
Preparation method Human embryonic kidney cells (HEK-293T) were transfected with wild-type (WT) or kinase inactive (KI) Myc-tagged ULK1 and wild-type Flag-tagged Vps34 (WT Vps34). 24 hours post-transfection, cells were treated with a panel of putative ULK1 competitive inhibitors in a dose response manner (1, 10, 50 μM). Cellular lysates were isolated after 1 hour of treatment and immunoblotted with the indicated antibodies.
Concentrations 1, 10, 50 μM
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 489.32
Formula C21H21BrN4O5
CAS Number 1884220-36-3
Purity 99.92%
Solubility 10 mM in DMSO
Storage at -20°C
References

SBI0206965, a novel inhibitor of Ulk1, suppresses non-small cell lung cancer cell growth by modulating both autophagy and apoptosis pathways.
Tang F, et al. Oncol Rep. 2017 Jun;37(6):3449-3458. PMID: 28498429.

Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.
Egan DF, et al. Mol Cell. 2015 Jul 16;59(2):285-97. PMID: 26118643.

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Keywords: SBI-0206965, SBI 0206965; SBI0206965 supplier, Autophagy, inhibitors

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