Cat. No.: HY-114490

ULK-101

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

ULK-101 is a potent and selective ULK1 inhibitor, with IC₅₀ values of 1.6 nM and 30 nM for ULK1 and ULK2, respectively. ULK-101 suppresses autophagy and sensitizes cancer cells to nutrient stress.

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Pureté: 99.91%
CAS No.: 2443816-45-1
Formule: C₂₂H₁₆F₄N₄OS
Masse moléculaire:460.45

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ULK-101 Chemical Structure

CAS No.: 2443816-45-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

ULK1

1.6 nM (IC₅₀)

ULK2

30 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform ULK :

ULK1
ULK2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	10 μM Compound: ULK-101	Cytotoxicity against human A549 cells harboring KRAS G12S mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay Cytotoxicity against human A549 cells harboring KRAS G12S mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay	[PMID: 30292171]
A549	EC₅₀	56.8 μM Compound: ULK-101	Cytotoxicity against human A549 cells harboring KRAS G12S mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo ass Cytotoxicity against human A549 cells harboring KRAS G12S mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo ass	[PMID: 30292171]
NCI-H2030	EC₅₀	20.3 μM Compound: ULK-101	Cytotoxicity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-gl Cytotoxicity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-gl	[PMID: 30292171]
NCI-H2030	EC₅₀	3.6 μM Compound: ULK-101	Cytotoxicity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay Cytotoxicity against human NCI-H2030 cells harboring KRAS G12C mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay	[PMID: 30292171]
NCI-H727	EC₅₀	25.6 μM Compound: ULK-101	Cytotoxicity against human NCI-H727 cells harboring KRAS G12V mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo Cytotoxicity against human NCI-H727 cells harboring KRAS G12V mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo	[PMID: 30292171]
NCI-H727	EC₅₀	3 μM Compound: ULK-101	Cytotoxicity against human NCI-H727 cells harboring KRAS G12V mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay Cytotoxicity against human NCI-H727 cells harboring KRAS G12V mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay	[PMID: 30292171]
NCI-H838	EC₅₀	1.2 μM Compound: ULK-101	Cytotoxicity against human NCI-H838 cells harboring KRAS mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay Cytotoxicity against human NCI-H838 cells harboring KRAS mutant assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay	[PMID: 30292171]
NCI-H838	EC₅₀	11.3 μM Compound: ULK-101	Cytotoxicity against human NCI-H838 cells harboring KRAS mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assa Cytotoxicity against human NCI-H838 cells harboring KRAS mutant assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assa	[PMID: 30292171]
U2OS	EC₅₀	22.3 μM Compound: ULK-101	Cytotoxicity against human U2OS cells assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability pretreated with compound for 2 days under full growth media condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay	[PMID: 30292171]
U2OS	EC₅₀	6.3 μM Compound: ULK-101	Cytotoxicity against human U2OS cells assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay Cytotoxicity against human U2OS cells assessed as reduction in cell viability pretreated with compound for 2 days under optistarve condition followed by replaced drug-free full growth media for 5 days by celltiter-glo assay	[PMID: 30292171]
U2OS	EC₅₀	700 nM Compound: ULK-101	Inhibition of autophagy in human U2OS cells assessed as BafA1-induced LC3B-II accumulation preincubated with compound for 3 hrs and followed by BafA1 induction and measured after 1.5 hrs by immunoblotting analysis Inhibition of autophagy in human U2OS cells assessed as BafA1-induced LC3B-II accumulation preincubated with compound for 3 hrs and followed by BafA1 induction and measured after 1.5 hrs by immunoblotting analysis	[PMID: 30292171]

In Vitro

ULK-101 (0-5 μM) reduces BafA1-induced LC3B-II accumulation in U2OS cells in a concentration-dependent manner^[1].

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

Chemical Information

CAS No. 2443816-45-1
Appearance Solid
Masse moléculaire 460.45
Formule C₂₂H₁₆F₄N₄OS
Color Light yellow to yellow
SMILES

FC1=CC=C(C(C=N2)=CN3C2=C(C4=CSC(C(N[C@@H](C5CC5)C(F)(F)F)=O)=C4)C=N3)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All WBFlow CytometryIn Vivo Efficacy Study

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Acta Pharmacol Sin

Semaglutide administration protects cardiomyocytes in db/db mice via energetic improvement and mitochondrial quality control. [Abstract]

2025 May;46(5):1250-1261. PMID: 39856432

ULK-101 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2025 May;46(5):1250-1261. [Abstract]

ULK1-101 (5 μM; 48 h) reversed semaglutide-induced hyperglycemia-induced mitophagy in primary mouse cardiomyocytes.
Cell Chem Biol

A nature-inspired nanoplatform for multi-protein targeted degradation via the autophagy-lysosome pathway. [Abstract]

2026 Apr 16;33(4):523-537.e7. PMID: 41932333
Cell Rep

Targeting the DSTYK-ULK1 axis rewires TNFR1 signaling to overcome treatment resistance in lung cancer. [Abstract]

2026 Mar 12;45(3):117087. PMID: 41824459

ULK-101 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Mar 12;45(3):117087. [Abstract]

Analysis of H2009 parental, parental treated with ULK1 inhibitor (ULK-101; 10 μM), and DSTYK KO Annexin V+ cells performed by cytometry under basal conditions or in the absence of glucose for 16 h.

ULK-101 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Mar 12;45(3):117087. [Abstract]

Cropped images from the western blot analysis of caspases (3 and 8) and p-MLKL in H2009 parental, parental treated with ULK1 inhibitor (ULK-101; ULK1inh;10 μM), and DSTYK KO cells under starvation conditions without glucose for 16 h.

ULK-101 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Mar 12;45(3):117087. [Abstract]

Subcutaneous xenograft mouse model for human H2009 lung adenocarcinoma. Once tumors were established and reached 50–75 mm3 (day 17 after inoculation), mice were randomized (n = 8), ULK1 was inhibited with ULK-101 inhibitor (100 nM) intravenously daily, and treated with carboplatin + paclitaxel combo.

ULK-101 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Mar 12;45(3):117087. [Abstract]

Subcutaneous syngeneic mouse model for human LLC lung adenocarcinoma. Once tumors were established and reached 50–75 mm3 (day 8 after inoculation), mice were randomized (n = 8), ULK1 was inhibited with ULK-101 inhibitor (200nM) intravenously daily, and treated with carboplatin+paclitaxel and anti-PD1 combo according to previous published regimens.
Mol Ther Oncolytics

Oleanolic acid blocks the purine salvage pathway for cancer therapy by inactivating SOD1 and stimulating lysosomal proteolysis. [Abstract]

2021 Aug 28:23:107-123. PMID: 34703880

ULK-101 purchased from MedChemExpress. Usage Cited in: Mol Ther Oncolytics. 2021 Aug 28:23:107-123. [Abstract]

The effects of two ULK1 inhibitors, ULK-101 (1 μM; 0, 3, 6, 8 h) and MRT68921 (1 μM), on levels of phospho-ATG14 (Ser29), ATG14, LC3-I/II, HGPRT, and 5′-NT in OA-treated A549 cells.
Int Immunopharmacol

The Lnc-Gm20716/miR-20b-5p/ULK1 axis regulates HDM-induced endoplasmic reticulum stress and Golgi fragmentation in mouse bronchial epithelial cells. [Abstract]

2025 Jun 17:161:115095. PMID: 40532330
Bioorg Med Chem

Design, synthesis and biological evaluation of benzimidazole carbamide derivatives - potential autophagy inducers. [Abstract]

2026 Jul:138:118646. PMID: 41934864
Università Vita-Salute San Raffaele

2022 Apr 08. 34.
The University of Chicago

Pritzker School of Medicine. 2021 Oct.

Solvant et solubilité

In Vitro:

DMSO : 83.33 mg/mL (180.98 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

2.1718 mL

10.8589 mL

21.7179 mL

5 mM

0.4344 mL

2.1718 mL

4.3436 mL

10 mM

0.2172 mL

1.0859 mL

2.1718 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 2.08 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[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. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1718 mL	10.8589 mL	21.7179 mL	54.2947 mL
	5 mM	0.4344 mL	2.1718 mL	4.3436 mL	10.8589 mL
	10 mM	0.2172 mL	1.0859 mL	2.1718 mL	5.4295 mL
	15 mM	0.1448 mL	0.7239 mL	1.4479 mL	3.6196 mL
	20 mM	0.1086 mL	0.5429 mL	1.0859 mL	2.7147 mL
	25 mM	0.0869 mL	0.4344 mL	0.8687 mL	2.1718 mL
	30 mM	0.0724 mL	0.3620 mL	0.7239 mL	1.8098 mL
	40 mM	0.0543 mL	0.2715 mL	0.5429 mL	1.3574 mL
	50 mM	0.0434 mL	0.2172 mL	0.4344 mL	1.0859 mL
	60 mM	0.0362 mL	0.1810 mL	0.3620 mL	0.9049 mL
	80 mM	0.0271 mL	0.1357 mL	0.2715 mL	0.6787 mL
	100 mM	0.0217 mL	0.1086 mL	0.2172 mL	0.5429 mL

Keywords

ULK-101

9 Cited Publications

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ULK-101

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Chemical Probe Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mouse Metabolite Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ULK-101

Voir tous les produits spécifiques à Isoform ULK

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ULK-101

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Chemical Probe Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mouse Metabolite Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) ULK-101

Voir tous les produits spécifiques à Isoform ULK

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

ULK-101 Related Classifications

HY-114490 Related Classifications