MKT-077 (Synonyms: FJ-776)

Name: MKT-077
Brand: MedChemExpress
SKU: HY-15096
Rating: 5.0 (16 reviews)

Cat. No.: HY-15096 Purity: 98.49%: Data Sheet
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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.

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

CAS No. : 147366-41-4

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 16 publication(s) in Google Scholar

16 Publications Citing Use of MCE MKT-077

In Vivo Imaging

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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.

: MKT-077 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2022 Jul 20;20(1):340. [Abstract]; Fluc imaging of ovarian cancer development in vivo. Representative mouse from distinct treatments is presented: (1) PBS. (2) EIPA. (3) Lovastatin. (4) Lovastatin + EIPA. (5) GCB. (6) GCB + EIPA. (7) Ro3306. (8) Ro3306 + EIPA. (9) PTX. (10) PTX + EIPA. (11) MKT077 (intratumoral injection, 7.5 mg/kg). (12) MKT077 + EIPA.

: 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).

: MKT-077 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2022 Jul 20;20(1):340. [Abstract]; TUNEL-assay-determined cellular apoptosis of ovarian tumors within different groups (MKT077 (intratumoral injection, 7.5 mg/kg); MKT077 + EIPA).

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]

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.

Molecular Weight

432.00

Formula

C₂₁H₂₂ClN₃OS₂

CAS No.

147366-41-4

Appearance

Solid

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-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-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)

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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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mg/kg

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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

Purity & Documentation

Purity: 98.49%

Select Batch:

Data Sheet (294 KB) SDS (393 KB)

COA (255 KB) HNMR (364 KB) RP-HPLC (265 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

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

MKT-077 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MKT-077147366-41-4FJ-776MKT077MKT 077FJ776FJ 776Fluorescent DyeHSPHeat shock proteinsInhibitorinhibitorinhibit

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MKT-077 (Synonyms: FJ-776)

Customer Review

MKT-077 Related Antibodies

16 Publications Citing Use of MCE MKT-077

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Customer Review

MKT-077 Related Antibodies

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Complete Stock Solution Preparation Table

MKT-077 Related Classifications

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