Cat. No.: HY-143466

ULK1-IN-2

Customer Review

Based on 1 Customer Validation

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC₅₀ of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).

For research use only. We do not sell to patients.

Purity: 98.34%
CAS No.: 2497409-01-3
Formula: C₁₉H₁₆BrFN₄O₆
Molecular Weight:495.26

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ULK1-IN-2 Chemical Structure

CAS No.: 2497409-01-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

ULK1

All ULK Isoforms :

ULK1
ULK2

All AMPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.94 μM Compound: 3s	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
HL-60	IC₅₀	10.89 μM Compound: 3s	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MCF7	IC₅₀	19.6 μM Compound: 3s	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
MDA-MB-468	IC₅₀	16.83 μM Compound: 3s	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]
U-937	IC₅₀	12.92 μM Compound: 3s	Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 32961380]

In Vitro

ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7^[1].
ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells^[1].
ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner^[1].
ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1^ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:

Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7^[1]
Concentration:

10 μM
Incubation Time:

24 h
Result:

Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC₅₀ values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.

Cell Autophagy Assay

Cell Line:

A549 cells^[1]
Concentration:

0, 2, 4, 8 μM
Incubation Time:

24 h
Result:

Blocked autophagy of A549 cells via inhibiting ULK.

Western Blot Analysis

Cell Line:

A549 cells^[1]
Concentration:

0, 2, 4, 8 μM
Incubation Time:

24 h
Result:

Inhibited expression of ULK1 and p-ULK1^ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.

Chemical Information

CAS No. 2497409-01-3
Appearance Solid
Molecular Weight 495.26
Formula C₁₉H₁₆BrFN₄O₆
Color Light yellow to yellow
SMILES

COC1=C(OC)C(OC)=CC(NC2=NC=C(Br)C(OC3=CC=C([N+]([O-])=O)C=C3F)=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (67.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0191 mL

10.0957 mL

20.1914 mL

5 mM

0.4038 mL

2.0191 mL

4.0383 mL

10 mM

0.2019 mL

1.0096 mL

2.0191 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sun D, Yang Z, Zhen Y, et al. Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer. Eur J Med Chem. 2020;208:112782. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0191 mL	10.0957 mL	20.1914 mL	50.4785 mL
	5 mM	0.4038 mL	2.0191 mL	4.0383 mL	10.0957 mL
	10 mM	0.2019 mL	1.0096 mL	2.0191 mL	5.0479 mL
	15 mM	0.1346 mL	0.6730 mL	1.3461 mL	3.3652 mL
	20 mM	0.1010 mL	0.5048 mL	1.0096 mL	2.5239 mL
	25 mM	0.0808 mL	0.4038 mL	0.8077 mL	2.0191 mL
	30 mM	0.0673 mL	0.3365 mL	0.6730 mL	1.6826 mL
	40 mM	0.0505 mL	0.2524 mL	0.5048 mL	1.2620 mL
	50 mM	0.0404 mL	0.2019 mL	0.4038 mL	1.0096 mL
	60 mM	0.0337 mL	0.1683 mL	0.3365 mL	0.8413 mL

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ULK1-IN-2

Apoptosis Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All ULK Isoforms

All AMPK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ULK1-IN-2 Related Classifications

Cat. No.: HY-143466