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MKT 077 (Synonyms: FJ-776)

Catalog No.GC17751

mortalin-2 (mot-2) inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

MKT 077 Chemical Structure

Cas No.: 147366-41-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$99.00
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1mg
$38.00
In stock
5mg
$90.00
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10mg
$162.00
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50mg
$450.00
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100mg
$585.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

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].

Animal experiment:

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].

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.
[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).
[3]. 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.

Background

MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity.

MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity. MKT-077 treatment (0.1 to 10 µM dose ranges) for 48 hours can effectively decrease TT cell viability. MKT-077 treatment results in accumulation of cells in the G0/G1 phase in a dose-dependent manner, and also increases sub-G0/G1 phase population in TT cell culture in a dose-dependent manner. MKT-077 also downregulates cellular levels of the proliferation marker, Ki67, and the S-phase transcription factor, E2F-1, in TT and MZ-CRC-1 cells. Moreover, flow cytometry using different doses of MKT-077 reveales that TT cells can uptake and retain MKT-077 at significantly higher levels than MZ-CRC-1 cells[1]. MKT-077 has EC50 values of 1.4±0.2 and 2.2±0.2 μM against MDA-MB-231 and MCF7 breast cancer cells, respectivelyl[2].

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].

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.
[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).
[3]. 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.

Chemical Properties

Cas No. 147366-41-4 SDF
Synonyms FJ-776
Chemical Name 1-ethyl-2-((Z)-((Z)-3-ethyl-5-(3-methylbenzo[d]thiazol-2(3H)-ylidene)-4-oxothiazolidin-2-ylidene)methyl)pyridin-1-ium chloride
Canonical SMILES O=C1N(CC)/C(S/C1=C2SC3=CC=CC=C3N\2C)=C/C4=CC=CC=[N+]4CC.[Cl-]
Formula C21H22ClN3OS2 M.Wt 432
Solubility DMSO: 2 mg/mL,Ethanol: 2 mg/mL,PBS (pH 7.2): 2 mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3148 mL 11.5741 mL 23.1481 mL
5 mM 0.463 mL 2.3148 mL 4.6296 mL
10 mM 0.2315 mL 1.1574 mL 2.3148 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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