Cat. No.: HY-100006

MRT68921

30 Cited Publications

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Based on 30 publication(s) in Google Scholar

MRT68921 is a potent NUAK1/ULK1 dual inhibitor. MRT68921 inhibits ULK1 and ULK2 with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. MRT68921 can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 can be used for the research of cancer, such as breast cancer.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 98.09%
CAS No.: 1190379-70-4
Formule: C₂₅H₃₄N₆O
Masse moléculaire:434.58

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MRT68921 Chemical Structure

CAS No.: 1190379-70-4

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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
- In Vitro
- In Vivo
Chemical Information
Publications (30)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]^[2]

ULK2

1.1 nM (IC₅₀)

ULK1

2.9 nM (IC₅₀)

GSK-3β

Bcl-2

Voir tous les produits spécifiques à Isoform ULK :

ULK1
ULK2

Voir tous les produits spécifiques à Isoform GSK-3 :

Voir tous les produits spécifiques à Isoform Bcl-2 Family :

In Vitro

MRT68921 (1 μM, 1 h) reduces basal LC3 puncta and blocks basal autophagy in mouse embryonic fibroblasts (MEFs)^[1].
MRT68921 (1 μM) reduces LC3-II levels in TBK1 knock-out and matched wild-type MEFs^[1].
MRT68921 (24 h) exhibits cytotoxic activity in cancer cells with IC₅₀ values ranging from 1.76-8.91 μM^[2].
MRT68921 (0-10 μM, 8-24 h) induces ROS production and apoptosis in NCI-H460 and MNK45 cells^[2].
MRT68921 (0-5 μM, 8h) suppresses the NUAK1/MYPT1/Gsk3β andautophagy associated signaling pathway in U251 and MNK45 cells^[2].

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

Western Blot Analysis^[1]

Cell Line:

U251 and MNK45 cells
Concentration:

0, 0.5, 1, 2, 3 and 5 μM
Incubation Time:

8 h
Result:

Increased cleaved PARP1 expression.
Downregulated phosphorylation of MYPT1 and Gsk3β.
Increased puncta LC3.

In Vivo

MRT68921 (10-40 mg/kg, s.c., daily for 7 times) inhibits tumor growth in NCI-H460 tumor mice models^[2].
MRT68921 (20 mg/kg, s.c., every 2 days for 7 times) inhibits tumor growth in MNK45 tumor mice models^[2].
MRT68921 (20 mg/kg, i.p., daily for 7 times) reduces the number of lung metastatic nodules in 4T1 tumor mice models^[2].

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

Animal Model:

NCI-H460 tumor mice models^[2]
Dosage:

10, 20, or 40 mg/kg
Administration:

Subcutaneously injection, daily for 7 times
Result:

Reduced tumor volume.
Increased Bax levels and decreased Bcl-2 levels.

Animal Model:

MNK45 tumor mice models^[2]
Dosage:

20 mg/kg
Administration:

Subcutaneously injection, every 2 days for 7 times
Result:

Reduced tumor volume.

Animal Model:

4T1 tumor mice models^[2]
Dosage:

20 mg/kg
Administration:

Intraperitoneally injection, daily for 7 times
Result:

Reduced the number of lung metastatic nodules.
Had no abnormal structures of the heart, kidney, liver, and spleen.

Chemical Information

CAS No. 1190379-70-4
Appearance Solid
Masse moléculaire 434.58
Formule C₂₅H₃₄N₆O
Color Light yellow to yellow
SMILES

O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (30)

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Journal Impact Factor

Nature

Collagenolysis-dependent DDR1 signalling dictates pancreatic cancer outcome. [Abstract]

2022 Oct;610(7931):366-372. PMID: 36198801
Cancer Cell

Cancer cells escape autophagy inhibition via NRF2-induced macropinocytosis. [Abstract]

2021 May 10;39(5):678-693.e11. PMID: 33740421
Nat Cancer

ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer. [Abstract]

2021 May;2(5):503-514. PMID: 34142094
Nat Cell Biol

TOLLIP targets GSDME-NT-carrying endocytic vesicles for autophagy to regulate pyroptosis and chemotherapy efficacy. [Abstract]

2026 Apr;28(4):812-827. PMID: 41803502
ACS Nano

Realistic Nanoplastics Induced Pulmonary Damage via the Crosstalk of Ferritinophagy and Mitochondrial Dysfunction. [Abstract]

2024 Jul 2;18(26):16790-16807. PMID: 38869479

MRT68921 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2024 Jul 2;18(26):16790-16807. [Abstract]

TC-1 cells were pretreated with 1 μM MRT68921 for 1 h, followed by NP treatment for 24 h. MRT68921 inhibited the upregulation of NP-induced p-ULK1, ATG5, and LC3-II and the downregulation of SQSTM1 and GPX4.
Nat Commun

PRDX1 promotes testosterone synthesis and attenuates aging via redox regulation of ATG4B to modulate lipophagy. [Abstract]

2025 Nov 19;16(1):10181. PMID: 41261096
J Exp Clin Cancer Res

Ferrodoxin 1 (FDX1) drives paclitaxel resistance in ovarian cancer via copper metabolism and ULK1/ATG13-mediated autophagy: overcome by pH/ROS-responsive PPD/PDP@si-FDX1 nanomicelles. [Abstract]

2026 Apr 23;45(1):104. PMID: 42026685
Cell Death Dis

Pictilisib and nutrient stress synergize to induce methuosis via PI(4,5)P2-dependent macropinocytic dysregulation in cancer cells. [Abstract]

2026 Jun 16. PMID: 42303628
Dev Cell

TM9SF3 is a Golgi-resident ATG8-binding protein essential for Golgi-selective autophagy. [Abstract]

2025 Jun 27:S1534-5807(25)00372-7. PMID: 40609542

MRT68921 purchased from MedChemExpress. Usage Cited in: Dev Cell. 2025 Jun 27:S1534-5807(25)00372-7. [Abstract]

Confocal images of mCherry-GOLPH3-expressing U2OS cells. Cells were either untreated or treated with EBSS for 12 hours, in the presence or absence of MRT68921 (250 μM). Right: Quantification of the percentage of cells with dispersed mCherry-GOLPH3. A total of 300 cells for each sample were quantified. n = 3. Scale bar: 10 µm.

MRT68921 purchased from MedChemExpress. Usage Cited in: Dev Cell. 2025 Jun 27:S1534-5807(25)00372-7. [Abstract]

Inhibition of EBSS-induced mCherry-GOLPH3 cleavage by ULK1 inhibitor MRT68921 (250 μM). U2OS cells transfected with the mCherry-GOLPH3 plasmid were left untreated or treated with EBSS, in the presence or absence of MRT68921 for 8 hours.
Dev Cell

Autophagy supports PDGFRA-dependent brain tumor development by enhancing oncogenic signaling. [Abstract]

2024 Jan 22;59(2):228-243.e7. PMID: 38113891
J Ethnopharmacol

Yunnan baiyao exerts anti-glioma activity by inducing autophagy-dependent necroptosis. [Abstract]

2024 Aug 3:118658. PMID: 39103023

MRT68921 purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2024 Aug 3:118658. [Abstract]

MRT68921 (MRT, 5 μM; 2 h) attenuates the accumulation of LC3-II, thereby reducing YB treatment-induced necroptosis.
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

MRT68921 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) and MRT68921 (1 μM), on levels of phospho-ATG14 (Ser29), ATG14, LC3-I/II, HGPRT, and 5′-NT in OA-treated A549 cells. The results showed that both ULK1 inhibitors rapidly downregulated phosphorylated ATG14 at Ser29, a well-established substrate of ULK1, reduced LC3-II isoform expression, and stabilized HGPRT and 5′-N.
PLoS Pathog

A small protein encoded by PCBP1-AS1 is identified as a key regulator of influenza virus replication via enhancing autophagy. [Abstract]

2024 Aug 13;20(8):e1012461. PMID: 39137200
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845
Biochem J

Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2). [Abstract]

2019 Mar 12;476(5):875-887. PMID: 30782972
FASEB J

EM2, a Novel Elephantopus mollis H.B.K. Monomer, Enhances Radiosensitivity in Cervical Cancer Through Dual Inhibition of AKT and Autophagy. [Abstract]

2026 Jan 31;40(2):e71454. PMID: 41527777
J Cell Physiol

αB-crystallin/HSPB2 is critical for hyperactive mTOR-induced cardiomyopathy. [Abstract]

2021 Dec;236(12):8110-8121. PMID: 34101831
Sci Rep

Autophagy dictates sensitivity to PRMT5 inhibitor in breast cancer. [Abstract]

2023 Jul 3;13(1):10752. PMID: 37400460
Med Oncol

ULK1-driven autophagy modulation alters tumor-promoting pathways in triple-negative breast cancer. [Abstract]

2026 Mar 3;43(4):163. PMID: 41774346
Mol Med Rep

Bif‑1 inhibits activation of inflammasome through autophagy regulatory mechanism. [Abstract]

2024 Apr;29(4):67. PMID: 38456519
mSphere

Inhibition of Unc-51-like-kinase is mitoprotective during Pseudomonas aeruginosa infection in corneal epithelial cells. [Abstract]

2025 Jan 10:e0053724. PMID: 39791872
Vet Microbiol

Porcine reproductive and respiratory syndrome virus nsp2 protects viral RNA-dependent RNA polymerase from autophagic degradation. [Abstract]

2026 May:316:110993. PMID: 41861694
bioRxiv

2026 Apr 5.
SSRN

2025 Jul 25.
bioRxiv

Leveraging autophagy and pyrimidine metabolism to target pancreatic cancer. [Abstract]

2025 Jun 5:2025.05.29.656904. PMID: 40501952
Res Sq

2025 May 07.
Medical University of South Carolina

2023 Aug 12.
Research Square Preprint

2023 May 22.
Patent

US20230068698A1.
Research Square Preprint

2021 Oct.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (230.11 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

2.3011 mL

11.5054 mL

23.0107 mL

5 mM

0.4602 mL

2.3011 mL

4.6021 mL

10 mM

0.2301 mL

1.1505 mL

2.3011 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: 2.5 mg/mL (5.75 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.75 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: 2.5 mg/mL (5.75 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (393 KB)
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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]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. [Content Brief]

[2]. Chen Y, et al. Dual targeting of NUAK1 and ULK1 using the multitargeted inhibitor MRT68921 exerts potent antitumor activities. Cell Death Dis. 2020 Sep 1;11(8):712. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3011 mL	11.5054 mL	23.0107 mL	57.5268 mL
	5 mM	0.4602 mL	2.3011 mL	4.6021 mL	11.5054 mL
	10 mM	0.2301 mL	1.1505 mL	2.3011 mL	5.7527 mL
	15 mM	0.1534 mL	0.7670 mL	1.5340 mL	3.8351 mL
	20 mM	0.1151 mL	0.5753 mL	1.1505 mL	2.8763 mL
	25 mM	0.0920 mL	0.4602 mL	0.9204 mL	2.3011 mL
	30 mM	0.0767 mL	0.3835 mL	0.7670 mL	1.9176 mL
	40 mM	0.0575 mL	0.2876 mL	0.5753 mL	1.4382 mL
	50 mM	0.0460 mL	0.2301 mL	0.4602 mL	1.1505 mL
	60 mM	0.0384 mL	0.1918 mL	0.3835 mL	0.9588 mL
	80 mM	0.0288 mL	0.1438 mL	0.2876 mL	0.7191 mL
	100 mM	0.0230 mL	0.1151 mL	0.2301 mL	0.5753 mL

MRT68921

30 Cited Publications

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MRT68921

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Antidepressant Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) MRT68921

Voir tous les produits spécifiques à Isoform ULK

Voir tous les produits spécifiques à Isoform GSK-3

Voir tous les produits spécifiques à Isoform Bcl-2 Family

Activité biologique

Chemical Information

Publications (30)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MRT68921 Related Classifications

HY-100006 Related Classifications