Free shipping on all orders over $ 500

SBI-0206965

Cat. No. M6086
SBI-0206965 Structure
Synonym:

SBI 0206965; SBI0206965

Size Price Availability Quantity
Free Sample 0.5 mg  USD 0 In stock
10mM*1mL in DMSO USD 80  USD80 In stock
2mg USD 50  USD50 In stock
5mg USD 75  USD75 In stock
10mg USD 125  USD125 In stock
50mg USD 380  USD380 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Product Citations
Protocol (for reference only)
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
Chemical Information
Molecular Weight 489.32
Formula C21H21BrN4O5
CAS Number 1884220-36-3
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Tang F, et al. Oncol Rep. SBI0206965, a novel inhibitor of Ulk1, suppresses non-small cell lung cancer cell growth by modulating both autophagy and apoptosis pathways.

[2] Egan DF, et al. Mol Cell. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.

Related ULK Products
MRT68921 

MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

SBP-7455

SBP-7455 is a dual-Specific ULK1/2 autophagy inhibitor with IC50s of 13 nM and 476 nM for ULK1 and ULK2 in ADP-Glo assay, respectively.

BL-918

BL-918 is a potent, orally active activator of UNC-51-like kinase 1 (ULK1) with EC50 of 24.14 nM and Kd of 0.719 μM. BL-918 induces cytoprotective autophagy for Parkinson's disease treatment.

MRT68921 dihydrochloride

MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

LYN-1604 dihydrochloride

LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).

  Catalog
Abmole Inhibitor Catalog




Keywords: SBI-0206965, SBI 0206965; SBI0206965 supplier, ULK, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.