SBI-0206965ULK1 inhibitor CAS# 1884220-36-3 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1884220-36-3 | SDF | Download SDF |
| PubChem ID | 92044402 | Appearance | Powder |
| Formula | C21H21BrN4O5 | M.Wt | 489.32 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (204.37 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[5-bromo-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]oxy-N-methylbenzamide | ||
| SMILES | CNC(=O)C1=CC=CC=C1OC2=NC(=NC=C2Br)NC3=CC(=C(C(=C3)OC)OC)OC | ||
| Standard InChIKey | NEXGBSJERNQRSV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H21BrN4O5/c1-23-19(27)13-7-5-6-8-15(13)31-20-14(22)11-24-21(26-20)25-12-9-16(28-2)18(30-4)17(10-12)29-3/h5-11H,1-4H3,(H,23,27)(H,24,25,26) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .
IC50 value: 108nM/711 nM
Target: ULK1/ ULK2
in vitro: 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. References: | |||||
SBI-0206965 Dilution Calculator
SBI-0206965 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0437 mL | 10.2183 mL | 20.4365 mL | 40.873 mL | 51.0913 mL |
| 5 mM | 0.4087 mL | 2.0437 mL | 4.0873 mL | 8.1746 mL | 10.2183 mL |
| 10 mM | 0.2044 mL | 1.0218 mL | 2.0437 mL | 4.0873 mL | 5.1091 mL |
| 50 mM | 0.0409 mL | 0.2044 mL | 0.4087 mL | 0.8175 mL | 1.0218 mL |
| 100 mM | 0.0204 mL | 0.1022 mL | 0.2044 mL | 0.4087 mL | 0.5109 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SBI-0206965 is a novel inhibitor of the autophagy-initiating kinase ULK1.
ULK1 (Unc-51 like Autophagy Activating Kinase 1) is a serine/threonine-protein kinase involved in autophagy in starvation. It is an AMPK regulator, a downstream effector and negative regulator of mTORC1. It also plays a role in neuronal differentiation. [1]
In A549 cells, 5 mM SBI-0206965 strongly suppresses the AZD8055 induced autophagy effect. In SBI-0206965 treated MEFs, after 18 hours of amino acid deprivation, 42% of 6965-treated cells shows 7-AAD and AnnexinV (end stage apoptosis). SBI-02066965 also promotes apoptosis
in the nutrient-starved state in human U87MG glioblastoma cells and in murine lung carcinoma cells. Moreover, 5 mM SBI-0206965 triggers apoptosis in 23% of cells when combined with AZD8055 versus 10% of cells in the absence of AZD8055 and 7% of cells treated with AZD8055
alone. Similar to AZD8055, both rapamycin and INK128 exhibits a mild apoptotic response on their own in A549 cells but significantly enhances this apoptotic response when combined with SBI-0206965. [1]
Reference:
1. Egan DF, Chun MG, Vamos M et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-97.
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Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.[Pubmed:26118643]
Mol Cell. 2015 Jul 16;59(2):285-97.
Many tumors become addicted to autophagy for survival, suggesting inhibition of autophagy as a potential broadly applicable cancer therapy. ULK1/Atg1 is the only serine/threonine kinase in the core autophagy pathway and thus represents an excellent drug target. Despite recent advances in the understanding of ULK1 activation by nutrient deprivation, how ULK1 promotes autophagy remains poorly understood. Here, we screened degenerate peptide libraries to deduce the optimal ULK1 substrate motif and discovered 15 phosphorylation sites in core autophagy proteins that were verified as in vivo ULK1 targets. We utilized these ULK1 substrates to perform a cell-based screen to identify and characterize a potent ULK1 small molecule inhibitor. The compound SBI-0206965 is a highly selective ULK1 kinase inhibitor in vitro and suppressed ULK1-mediated phosphorylation events in cells, regulating autophagy and cell survival. SBI-0206965 greatly synergized with mechanistic target of rapamycin (mTOR) inhibitors to kill tumor cells, providing a strong rationale for their combined use in the clinic.
