Cat. No.: HY-184501

UE01

Name: UE01
Brand: MedChemExpress
SKU: HY-184501
Price: 115.00 USD
Availability: InStock
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Based on 1 Customer Validation

UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC₅₀ of 695.30 nM and a K_D of 114.3 nM for ULK1; it inhibits hERK1 with an IC₅₀ of 179.90 nM and a K_D of 114 nM for ERK1; it shows weak binding to ERK2 with a K_D of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer.

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

Purity : 99.70%
CAS No.: 486440-74-8
Formula: C₁₈H₁₃BrCl₂N₂O₂
Molecular Weight:440.12

Storage:

4°C, sealed storage, away from moisture

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

UE01 Chemical Structure

CAS No.: 486440-74-8

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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
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

hULK1

695.3 nM (EC₅₀)

ULK1

114.3 nM (Kd, SPR)

hERK1

179.9 nM (IC₅₀)

erk1

114 nM (Kd, SPR)

ERK2

2.8 mM (Kd, SPR)

All ULK Isoforms :

ULK1
ULK2

All ERK Isoforms :

All Bcl-2 Family Isoforms :

All MMP Isoforms :

In Vitro

OthersAnti-cancerAutophagy

Others

UE01 activates human ULK1 with an EC₅₀ of 695.30 nM, and inhibits ERK1 with an IC₅₀ of 179.90 nM; the K_d values of UE01 for ULK1, ERK1 and ERK2 are 114.3 nM, 114 nM and 2.8 mM, respectively^[1].
UE01 (20 μM; 6 h) increases the thermal stability and protease degradation resistance of ULK1, ERK1 and ERK2 in MDA-MB-231 cells, induces activation-associated conformational changes in ULK1, and competitively occupies the ATP-binding pocket of ERK1^[1].

Anti-cancer

UE01 inhibits the proliferation of triple-negative breast cancer cells MDA-MB-231 and BT-549, with IC₅₀ values of 21.86 μM and 24.24 μM, respectively^[1].
UE01 (10-40 μM; 24 h) upregulates E-cadherin, downregulates MMP-2, MMP-9 and Cav-1, and reduces the phosphorylation level of Exo70 Ser250, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation^[1].
UE01 (20 μM; 48 h) significantly inhibits the migration of MDA-MB-231 and BT-549 cells in scratch wound healing assays, with stronger efficacy than single-target controls, and this effect is mediated by activating ULK1 and inhibiting ERK1/2/Exo70^[1].
UE01 (20 μM; 48 h) significantly inhibits the migration of MDA-MB-231 cells in Transwell assays, with stronger efficacy than single-target controls, and this effect depends on the expression of ULK1 and ERK1^[1].
UE01 (10-40 μM; 24 h) activates the ULK1 signaling pathway and inhibits the ERK1/2 signaling pathway in a concentration-dependent manner, and regulates metastasis-related proteins (upregulates E-cadherin, downregulates Cav-1, MMP-2, MMP-9) in MDA-MB-231 and BT-549 cells. These effects are mediated by the ULK1 and Cav-1/Exo70 pathways^[1].
UE01 (20 μM; 24 h) upregulates the expression of E-cadherin and downregulates the expression of MMP-2 in MDA-MB-231 cells, and its downregulatory effect on MMP-2 is stronger than that of the single-target control^[1].

Autophagy

UE01 (10-40 μM; 24 h) increases autophagy levels in MDA-MB-231 and BT-549 cells in a concentration-dependent manner, as determined by LC3B fluorescence assay^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231, BT-549 triple-negative breast cancer cells
Concentration:

10, 20, 40 μM
Incubation Time:

24 h
Result:

Concentration-dependently increased ULK1 protein abundance, phosphorylation of ULK1 (Ser317) and mAtg13 (Ser355), and E-cadherin expression in MDA-MB-231 cells.
Concentration-dependently decreased phosphorylation of ULK1 (Ser757), p-MAPK1/3 (Thr202/Tyr204), Cav-1, MMP-2, and MMP-9 expression in MDA-MB-231 cells, with no change in upstream MAPK components (Ras, c-Raf, p-c-Raf, MEK1/2, p-MEK1/2).
Concentration-dependently increased E-cadherin expression and decreased MMP-2 expression in BT-549 cells.
Had its effects on Exo70, MMP-2, and E-cadherin expression attenuated by ULK1 knockdown.
Had its inhibitory effects on MMP-2 and p-Exo70 (Ser250), and stimulatory effect on E-cadherin reversed by overexpression of Cav-1.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 triple-negative breast cancer cells
Concentration:

10, 20, 40 μM
Incubation Time:

24 h
Result:

Concentration-dependently increased Atg5, Atg7, and LC3-II/LC3-I ratio.
Concentration-dependently decreased p62 expression.

Immunofluorescence^[1]

Cell Line:

MDA-MB-231, BT-549 triple-negative breast cancer cells
Concentration:

10, 20, 40 μM
Incubation Time:

24 h
Result:

Concentration-dependently increased LC3B fluorescence intensity in both cell lines.

Cell Autophagy Assay^[1]

Cell Line:

MDA-MB-231 triple-negative breast cancer cells
Concentration:

10, 20, 40 μM
Incubation Time:

24 h
Result:

Concentration-dependently increased MDC fluorescence intensity, indicating enhanced autophagic activity.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231,
Concentration:

20 μM
Incubation Time:

24 h
Result:

Increased the proportions of early and late apoptotic cells and produced a greater total apoptosis rate than the control and LYN-1604 groups.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	Bioavailability
Rat^[1]	5 mg/kg	i.v.	0.61 h	0.08 h	2016.15 ng/mL	821.90 ng·h/mL	825.32 ng·h/mL	/
Rat^[1]	50 mg/kg	p.o.	1.09 h	0.85 h	1544.14 ng/mL	3064.31 ng·h/mL	3069.56 ng·h/mL	26.78 %

In Vivo

Anti-cancerOthers

Anti-cancer

UE01 (25-100 mg/kg; p.o.; once daily; for 13 consecutive days) dose-dependently inhibits tumor growth, reduces tumor volume, tumor weight and bioluminescent signals, downregulates Ki-67 and p-ERK1/2, and upregulates p-ULK1 in the MDA-MB-231-Luc subcutaneous xenograft tumor model^[1].
UE01 (25-100 mg/kg; p.o.; once daily; for 13 consecutive days) dose-dependently reduces pulmonary bioluminescent signals and the number of lung metastatic nodules, upregulates E-cadherin, downregulates MMP-2, and improves collagen fiber structure in the MDA-MB-231-Luc tail vein lung metastasis model^[1].

Others

UE01 (25-100 mg/kg; p.o.; once daily; for 13 consecutive days) does not significantly alter body weight or serum indicators of liver and kidney function in mice, but histopathological lesions are observable in liver tissues of the high-dose group^[1].

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

Animal Model:

BALB/c nude (male, 20-22 g, subcutaneous xenograft model)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

p.o.; daily; 13 days
Result:

Dose-dependently reduced tumor volume, tumor weight and tumor bioluminescence.
Reduced Ki-67, p-ERK1/2 and MMP-2 staining, increased p-ULK1 and E-cadherin staining, and increased collagen volume fraction in tumor tissues.
Did not significantly alter body weight or serum liver and renal function biomarkers, although liver histopathological lesions were observed in the 100 mg/kg group.

Animal Model:

BALB/c nude (male, 20-22 g, lung metastasis model)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

p.o.; daily; 13 days
Result:

Dose-dependently reduced pulmonary bioluminescence and the number of pulmonary metastatic nodules.
Increased continuous peritumoral collagen deposition, reduced collagen degradation, produced a clearer tumor-stroma interface and better preserved adjacent pulmonary architecture.

Related Protocols :

Chemical Information

CAS No. 486440-74-8
Appearance Solid
Molecular Weight 440.12
Formula C₁₈H₁₃BrCl₂N₂O₂
SMILES

O=C(OC(C1=CC=C(Cl)C=C1Cl)CN2C=CN=C2)C3=CC=C(Br)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (227.21 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

2.2721 mL

11.3605 mL

22.7211 mL

5 mM

0.4544 mL

2.2721 mL

4.5442 mL

10 mM

0.2272 mL

1.1361 mL

2.2721 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). 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)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

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]. Liao MR, et al. Discovery of a novel dual-target modulator of ULK1 and ERK1/2 that suppresses triple-negative breast cancer progression and metastasis via the Exo70/Cav-1/MMPs axis. Acta pharmacologica Sinica. 2026 Jun 01. [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	2.2721 mL	11.3605 mL	22.7211 mL	56.8027 mL
	5 mM	0.4544 mL	2.2721 mL	4.5442 mL	11.3605 mL
	10 mM	0.2272 mL	1.1361 mL	2.2721 mL	5.6803 mL
	15 mM	0.1515 mL	0.7574 mL	1.5147 mL	3.7868 mL
	20 mM	0.1136 mL	0.5680 mL	1.1361 mL	2.8401 mL
	25 mM	0.0909 mL	0.4544 mL	0.9088 mL	2.2721 mL
	30 mM	0.0757 mL	0.3787 mL	0.7574 mL	1.8934 mL
	40 mM	0.0568 mL	0.2840 mL	0.5680 mL	1.4201 mL
	50 mM	0.0454 mL	0.2272 mL	0.4544 mL	1.1361 mL
	60 mM	0.0379 mL	0.1893 mL	0.3787 mL	0.9467 mL
	80 mM	0.0284 mL	0.1420 mL	0.2840 mL	0.7100 mL
	100 mM	0.0227 mL	0.1136 mL	0.2272 mL	0.5680 mL

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UE01

All ULK Isoforms

All ERK Isoforms

All Bcl-2 Family Isoforms

All MMP Isoforms