Cat. No.: HY-15096

MKT-077

(Synonyms: FJ-776)

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity. MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm.

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Pureté: 98.49%
CAS No.: 147366-41-4
Formule: C₂₁H₂₂ClN₃OS₂
Masse moléculaire:432.00

Stockage:

-20°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)

MKT-077 Chemical Structure

CAS No.: 147366-41-4

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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
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (18)
Solvant et solubilité
- In Vitro
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity^[1]. MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm^[2].

IC₅₀ & Target^[1]

HSP70

Voir tous les produits spécifiques à Isoform HSP :

Cellular Effect

Cell Line	Type	Value	Description	References
Cancer cell lines	IC₅₀	1 μM Compound: 31, MKT-077	Antiproliferative activity against human bladder cancer cells Antiproliferative activity against human bladder cancer cells	[PMID: 20334364]
Cancer cell lines	IC₅₀	1 μM Compound: 31, MKT-077	Antiproliferative activity against human breast cancer cells Antiproliferative activity against human breast cancer cells	[PMID: 20334364]
Cancer cell lines	IC₅₀	1 μM Compound: 31, MKT-077	Antiproliferative activity against human colon cancer cells Antiproliferative activity against human colon cancer cells	[PMID: 20334364]
CX-1	IC₅₀	0.81 μM Compound: 3	In vitro inhibition of growth of human carcinoma CX-1 cell line (clonogenic assay). In vitro inhibition of growth of human carcinoma CX-1 cell line (clonogenic assay).	[PMID: 9438030]
FM3A	EC₅₀	1.5 x 10^-5 M Compound: MKT-077	Cytotoxicity against mouse mammary tumor FM3A cells representing a model of host Cytotoxicity against mouse mammary tumor FM3A cells representing a model of host	[PMID: 11855978]
KB	IC₅₀	>69 μM Compound: 3	In vitro inhibition of growth of KB cells (cytotoxic assay). In vitro inhibition of growth of KB cells (cytotoxic assay).	[PMID: 9438030]
L6	IC₅₀	114.8 μM Compound: 1, MKT-077	Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 19894726]
MCF7	EC₅₀	2.2 μM Compound: MKT-077	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24312699]
MDA-MB-231	EC₅₀	1.4 μM Compound: MKT-077	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24312699]
MEF	EC₅₀	>50 μM Compound: MKT-077	Cytotoxicity against C57BL/6 mouse MEF assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against C57BL/6 mouse MEF assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 24312699]
NCI-H460	IC₅₀	1.3 μM Compound: MKT-077	Antitumor activity against human NCI-H460 cells Antitumor activity against human NCI-H460 cells	[PMID: 31926469]
NCI-H460	IC₅₀	1.3 μM/L Compound: MKT-077	Antitumor activity against human NCI-H460 cells Antitumor activity against human NCI-H460 cells	[PMID: 31926469]

In Vitro

Guide (The following is our recommended protocol. This protocol is only a guide and should be modified according to your specific needs).
Preparation of MKT-077 solution
1.1 Preparation of the stock solution
Dissolve 1 mg MKT-077 in 0.2315 mL DMSO to obtain 10 mM of MKT-077 .
Note: It is recommended to store the stock solution at -20 °C -80 °C away from light and avoid repetitive freeze-thaw cycles.
1.2 Preparation of MKT-077 working solution
Dilute the stock solution in serum-free cell culture medium or PBS to obtain 5-10 μM of MKT-077 working solution.
Note: Please adjust the concentration of MKT-077 working solution according to the actual situation.

Cell staining
2.1 Cell preparation.
For suspension cells: Centrifuge at 1000 g at 4°C for 3-5 minutes and then discard the supernatant. Wash twice with PBS, 5 minutes each time.
For adherent cells: Discard the cell culture medium, and add trypsin to dissociate cells to make a single-cell suspension. Centrifuge at 1000 g at 4°C for 3-5 minutes and then discard the supernatant. Wash twice with PBS, 5 minutes each time.
2.2 Add 1 mL of MKT-077 working solution, and then incubate at room temperature for 30 minutes.
2.3 Centrifuge at 400 g at 4°C for 3-4 minutes and then discard the supernatant.
2.4 Wash twice with PBS, 5 minutes each time.
2.5 Resuspend cells with serum-free cell culture medium or PBS, and then detect by fluorescence microscope or flow cytometer.

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

In Vivo

Systemic administration of MKT-077 significantly delays the growth of TT xenografts in mice throughout the treatment. At the end of MKT-077 treatment, it is found that tumor weights are about two-times less in MKT-077-treated group than in control group. MKT-077 treatment also results in weight loss and general toxicity in animals^[1]. Results show that the succinate-induced, ADP-stimulated respiratory rate in mitochondria isolated from the liver of rats treated with a bolus i.v. injection of 15 mg MKT-077 1kg body weight each day for 5 days is significantly lower than that of untreated controls^[3].

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

Chemical Information

CAS No. 147366-41-4
Appearance Solid
Masse moléculaire 432.00
Formule C₂₁H₂₂ClN₃OS₂
Color Brown to reddish brown
SMILES

CN(C1=CC=CC=C1S/2)C2=C3C(N(CC)/C(S\3)=C/C4=[N+](CC)C=CC=C4)=O.[Cl-]
Synonyms

FJ-776
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-20°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)

Publications (18)

All WBBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

Nat Cell Biol

ERO1a fosters glioblastoma aggressiveness and metabolic flexibility by regulating mitochondria-associated membrane dynamics. [Abstract]

2026 Jun 12. PMID: 42286227
J Nanobiotechnology

GRP75-driven, cell-cycle-dependent macropinocytosis of Tat/pDNA-Ca2+ nanoparticles underlies distinct gene therapy effect in ovarian cancer. [Abstract]

2022 Jul 20;20(1):340. PMID: 35858873

MKT-077 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2022 Jul 20;20(1):340. [Abstract]

Body weight of the ovarian tumors at 21 day post-administration with Tat/TF-Ca²⁺ nanoparticles and treatments with different inhibitors (MKT077 (intratumoral injection, 7.5 mg/kg); MKT077 + EIPA).
Cell Death Dis

A common druggable signature of oncogenic c-Myc, mutant KRAS and mutant p53 reveals functional redundancy and competition among oncogenes in cancer. [Abstract]

2024 Aug 31;15(8):638. PMID: 39217152
J Transl Med

TRPA1 promotes cisplatin-induced acute kidney injury via regulating the endoplasmic reticulum stress-mitochondrial damage. [Abstract]

2023 Oct 5;21(1):695. PMID: 37798747

MKT-077 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 5;21(1):695. [Abstract]

The ERS-related proteins GRP78, CHOP, and GRP75 levels in HK-2 cells were measured using western blot. Control: left untreated; TRPA1 agonists: 100 µM AITC for 24 h; TRPA1 agonists+ERS inhibitor: 100 µM AITC and 1 mM 4-PBA for 24 h; TRPA1 agonists+GRP75 inhibitor: 100 µM AITC and 1 µM MKT077 for 24 h.

MKT-077 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 5;21(1):695. [Abstract]

ERS inhibitors and GRP75 inhibitors reduced the cisplatin-induced up-regulation of Ca²⁺ concentration in HK-2 cells. TRPA1 agonists: 100 µM AITC for 24 h; TRPA1 agonists+ERS inhibitor: 100 µM AITC and 1 mM 4-PBA for 24 h; TRPA1 agonists+GRP75 inhibitor: 100 µM AITC and 1 µM MKT077 for 24 h.
Dev Cell

GRP75-dependent mitochondria-ER contacts ensure cell survival during early mouse thymocyte development. [Abstract]

2024 Jul 3:S1534-5807(24)00385-X. PMID: 38981469
Int J Surg

Intelligent identification and targeted intervention of GRP75-caused drug resistant hepatocellular carcinoma, a study based on radiomics, machine learning, and molecular pharmacology. [Abstract]

2026 Feb 19. PMID: 41711200
Int J Biol Macromol

A kinase-independent Bcr-Abl function mediating an Hsp70-Bim protein-protein interaction in chronic myeloid leukemia. [Abstract]

2025 Apr 16:143249. PMID: 40250683
Atherosclerosis

GRP75 inhibition attenuates arterial calcification. [Abstract]

2025 May 15:119243. PMID: 40410081
Virulence

Differential roles of HSP70 and HSP90 in Senecavirus A infection: IRES-dependent translational regulation and viral replication mechanisms. [Abstract]

2026 Dec;17(1):2605380. PMID: 41412139
Eur J Med Chem

A novel Hsp70 inhibitor specifically targeting the cancer-related Hsp70-Bim protein-protein interaction. [Abstract]

2021 Aug 5:220:113452. PMID: 33906046
Cell Biosci

ApoE4 (Δ272-299) induces mitochondrial-associated membrane formation and mitochondrial impairment by enhancing GRP75-modulated mitochondrial calcium overload in neuron. [Abstract]

2021 Mar 6;11(1):50. PMID: 33676568
Pharm Biol

Aspirin relieves the calcification of aortic smooth muscle cells by enhancing the heat shock response. [Abstract]

2022 Dec;60(1):17-24. PMID: 34846265
Mol Oncol

Patient therapy outcome modeling in cancer organoids is improved by cancer-associated fibroblasts and organoid assembly convolution. [Abstract]

2026 Jun 5. PMID: 42246237
Front Biosci (Landmark Ed)

Maintenance of the Expression of c-FLIPL by Hsp70 to Resist Licochalcone A-Induced Anti-Colorectal Cancer Effect through ERK-Mediated Autophagy Induction. [Abstract]

2023 Dec 1;28(12):325. PMID: 38179732
bioRxiv

2025 Nov 18.
Research Square Print

2025 May 28.
bioRxiv

2023 Dec 21.
Research Square Preprint

2023 May 22.

Solvant et solubilité

In Vitro:

DMSO : 56.67 mg/mL (131.18 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

2.3148 mL

11.5741 mL

23.1481 mL

5 mM

0.4630 mL

2.3148 mL

4.6296 mL

10 mM

0.2315 mL

1.1574 mL

2.3148 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.

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)

Protocole

Cell Assay^[1]

Cells are incubated with 1 µM MKT-077 and 100 nM Mitotracker Green FM in culture medium for 30 minutes at 37°C in the dark, washed with PBS, switched into phenol-red free medium before visualizing fluorescence under a microscope. Pictures are acquired and processed with software. For flow cytometric measurement, MKT-077-treated cells are resuspended in 0.1% bovine serum albumin/PBS and analyzed by flow cytometry. Data from 20,000 cells are analyzed using FCS Express software^[1].

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

Animal Administration^[1]

The 1×10⁷ TT cells in 200 µL Hank's balanced salt solution are inoculated subcutaneously into the rear flanks of 6-week-old female athymic nude (nu/nu) mice. Once palpable, tumors are measured using calipers at intervals indicated in the text. When tumor volume reaches 100 mm³, mice are sorted into groups of 8 to achieve equal distribution of tumor size in all treatment groups. Group 1 receives only the vehicle (1:9 mixture of DMSO/saline) and group 2 receives MKT-077 (10 mg/kg body weight/dose). A 200 µL of ether solution is administered by intraperitoneal injection every 2 days (total 10 doses). At the end of the experiments, animals are euthanized by CO₂ asphyxiation^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (294 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Starenki D, et al. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. [Content Brief]

[2]. Li X, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013 Nov 14;4(11).. [Content Brief]

[3]. Starenki D, et al. Selective Mitochondrial Uptake of MKT-077 Can Suppress Medullary Thyroid Carcinoma Cell Survival In Vitro and In Vivo. Endocrinol Metab (Seoul). 2015 Dec;30(4):593-603. [Content Brief]

[4]. Li X, et al. Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents. ACS Med Chem Lett. 2013 Nov 14;4(11). [Content Brief]

[5]. Weisberg EL, et al. In vivo administration of MKT-077 causes partial yet reversible impairment of mitochondrial function. Cancer Res. 1996 Feb 1;56(3):551-5. [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	2.3148 mL	11.5741 mL	23.1481 mL	57.8704 mL
	5 mM	0.4630 mL	2.3148 mL	4.6296 mL	11.5741 mL
	10 mM	0.2315 mL	1.1574 mL	2.3148 mL	5.7870 mL
	15 mM	0.1543 mL	0.7716 mL	1.5432 mL	3.8580 mL
	20 mM	0.1157 mL	0.5787 mL	1.1574 mL	2.8935 mL
	25 mM	0.0926 mL	0.4630 mL	0.9259 mL	2.3148 mL
	30 mM	0.0772 mL	0.3858 mL	0.7716 mL	1.9290 mL
	40 mM	0.0579 mL	0.2894 mL	0.5787 mL	1.4468 mL
	50 mM	0.0463 mL	0.2315 mL	0.4630 mL	1.1574 mL
	60 mM	0.0386 mL	0.1929 mL	0.3858 mL	0.9645 mL
	80 mM	0.0289 mL	0.1447 mL	0.2894 mL	0.7234 mL
	100 mM	0.0231 mL	0.1157 mL	0.2315 mL	0.5787 mL

Keywords

MKT-077

18 Cited Publications

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MKT-077

Publications Citing Use of MedChemExpress (MCE) MKT-077

Voir tous les produits spécifiques à Isoform HSP

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MKT-077 Related Classifications

HY-15096 Related Classifications