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ULK-101

Catalog No. T5403 CAS 2443816-45-1

ULK-101 is a potent and selective ULK1 inhibitor ( IC50s: 8.3/30 nM for ULK1/ULK2). It can suppress autophagy.

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ULK-101, CAS 2443816-45-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 165.00
2 mg	In stock	$ 242.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 597.00
25 mg	In stock	$ 935.00
50 mg	In stock	$ 1,260.00
100 mg	In stock	$ 1,690.00
500 mg	In stock	$ 3,380.00
1 mL * 10 mM (in DMSO)	In stock	$ 377.00

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Purity: 99.66%

Purity: 99.51%

Purity: 98.05%

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Description	ULK-101 is a potent and selective ULK1 inhibitor ( IC50s: 8.3/30 nM for ULK1/ULK2). It can suppress autophagy.
Targets&IC50	ULK2:30 nM (cell free), ULK1:8.3 nM (cell free)
In vitro	U2OS cells were treated with AZD8055 for 2.5 hr, a catalytic mTOR inhibitor that strongly induces autophagy in U2OS cells and observed that the abundance of DFCP1-positive puncta increased over 3-fold. Co-treatment of cells with 5 μM ULK-101 completely abrogated the formation of DFCP1-positive structures induced by AZD8055 treatment, consistent with the loss of Beclin 1 phosphorylation.
Kinase Assay	IC50 data for ULK1 and ULK2 was generated using 10-point IC50Profiler assays with half-log dilutions from top concentrations of 10 μM (4 replicates) and 1 μM (4 replicates), giving 8 data points for most concentrations in the curve. For selectivity profiling, KinaseProfiler assays with wild-type human kinase panels were performed in duplicate using 500 nM SBI-0206965, 40 nM ULK-101, or 15 nM ULK-100. For each kinase reaction, the Km concentration of ATP was used. The percent activity remaining and percent inhibition were calculated from negative control wells. For selectivity profiling, relative inhibition was calculated by dividing the percent inhibition of each kinase by the percent inhibition of ULK1. GraphPad Prism 7 was used for IC50 determinations by fitting curves with variable slope (four-parameter) non-linear regression models using top and bottom constraints of 100% and 0%, respectively.
Cell Research	Cells (U2OS or NSCLC) were seeded on tissue culture treated 96-well plates at 1,000 cells per well in RPMI-1640 media supplemented with 10% FBS. Twenty-four hours later, media was aspirated, wells rinsed with 1x DPBS, and replaced with full media (FM) or Optistarve (OS) with a concentration gradient of ULK-101 (final concentrations of 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.1 μM, 1.6 μM, 0.8 μM, 0.4 μM, or 0 μM). Two days later, media (and ULK-101) was aspirated, wells were rinsed with 1x DPBS, and all wells replaced with FM. Five days later, relative ATP levels were measured using a luminescent CellTiter-Glo assay.

Molecular Weight	460.45
Formula	C22H16F4N4OS
CAS No.	2443816-45-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (173.74 mM)

H2O: Insoluble

References and Literature

1. Martin KR, et al. A Potent and Selective ULK1 Inhibitor Suppresses Autophagy and Sensitizes Cancer Cells to Nutrient Stress. iScience. 2018 Oct 26;8:74-84. 2. Xia Z, Zhang X, Liu P, et al. GNA13 regulates BCL2 expression and the sensitivity of GCB-DLBCL cells to BCL2 inhibitors in a palmitoylation-dependent manner[J]. Cell Death & Disease. 2021, 12(1): 1-11.

Citations

1. Xia Z, Zhang X, Liu P, et al. GNA13 regulates BCL2 expression and the sensitivity of GCB-DLBCL cells to BCL2 inhibitors in a palmitoylation-dependent manner. Cell Death & Disease. 2021, 12(1): 1-11.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Autophagy Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

ULK-101 2443816-45-1 Autophagy Unc-51 like kinase ULK ULK 101 Inhibitor inhibit ULK101 inhibitor

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