MRT68921 dihydrochloride

Name: MRT68921 dihydrochloride
Brand: MedChemExpress
SKU: HY-100006A
Rating: 5.0 (27 reviews)

Cat. No.: HY-100006A Purity: 99.67%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 2080306-21-2

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 27 publication(s) in Google Scholar

Other Forms of MRT68921 dihydrochloride:

MRT68921 In-stock
MRT68921 hydrochloride 견적 받기
MRT68921 dihydrochloride (Standard) 견적 받기

27 Publications Citing Use of MCE MRT68921 dihydrochloride

: MRT68921 dihydrochloride 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 dihydrochloride 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.

: MRT68921 dihydrochloride 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.

: MRT68921 dihydrochloride 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.

: MRT68921 dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Ther Oncolytics. 2021 Aug 28:23:107-123.; 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.

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ULK1 ULK2

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GSK-3 GSK-3α GSK-3β

View All Bcl-2 Family Isoform Specific Products:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]^[2]

ULK2

1.1 nM (IC₅₀)

ULK1

2.9 nM (IC₅₀)

GSK-3β

Bcl-2

In Vitro

MRT68921 dihydrochloride (1 μM, 1 h) reduces basal LC3 puncta and blocks basal autophagy in mouse embryonic fibroblasts (MEFs)^[1].
MRT68921 dihydrochloride (1 μM) reduces LC3-II levels in TBK1 knock-out and matched wild-type MEFs^[1].
MRT68921 dihydrochloride (24 h) exhibits cytotoxic activity in cancer cells with IC₅₀ values ranging from 1.76-8.91 μM^[2].
MRT68921 dihydrochloride (0-10 μM, 8-24 h) induces ROS production and apoptosis in NCI-H460 and MNK45 cells^[2].
MRT68921 dihydrochloride (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 dihydrochloride (10-40 mg/kg, s.c., daily for 7 times) inhibits tumor growth in NCI-H460 tumor mice models^[2].
MRT68921 dihydrochloride (20 mg/kg, s.c., every 2 days for 7 times) inhibits tumor growth in MNK45 tumor mice models^[2].
MRT68921 dihydrochloride (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.

분자량

507.50

화학식

C₂₅H₃₆Cl₂N₆O

CAS No.

2080306-21-2

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

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

용액&용해도

In Vitro:

H₂O : 20.83 mg/mL (41.04 mM; ultrasonic and warming and heat to 60°C)

DMSO : 8.33 mg/mL (16.41 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9704 mL	9.8522 mL	19.7044 mL
5 mM	0.3941 mL	1.9704 mL	3.9409 mL
10 mM	0.1970 mL	0.9852 mL	1.9704 mL

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

순도&문서

Purity: 99.67%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.9704 mL	9.8522 mL	19.7044 mL	49.2611 mL
	5 mM	0.3941 mL	1.9704 mL	3.9409 mL	9.8522 mL
	10 mM	0.1970 mL	0.9852 mL	1.9704 mL	4.9261 mL
	15 mM	0.1314 mL	0.6568 mL	1.3136 mL	3.2841 mL
H₂O	20 mM	0.0985 mL	0.4926 mL	0.9852 mL	2.4631 mL
	25 mM	0.0788 mL	0.3941 mL	0.7882 mL	1.9704 mL
	30 mM	0.0657 mL	0.3284 mL	0.6568 mL	1.6420 mL
	40 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2315 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.