MKT 077
Modify Date: 2024-01-09 09:24:39
MKT 077 structure
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Common Name | MKT 077 | ||
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| CAS Number | 147366-41-4 | Molecular Weight | 432.00200 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H22ClN3OS2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of MKT 077MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity. |
| Name | 3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one,chloride |
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| Synonym | More Synonyms |
| Description | MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity. |
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| Related Catalog | |
| Target |
HSP70 |
| In Vitro | 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]. |
| 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]. |
| Cell Assay | 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 Admin | 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 |
| Molecular Formula | C21H22ClN3OS2 |
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| Molecular Weight | 432.00200 |
| Exact Mass | 431.08900 |
| PSA | 87.29000 |
| LogP | 0.19120 |
| Storage condition | -20℃ |
| RIDADR | NONH for all modes of transport |
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| RTECS | UU4023332 |
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Toll receptors type-2 and CR3 expression of canine monocytes and its correlation with immunohistochemistry and xenodiagnosis in visceral leishmaniasis.
PLoS ONE 6 , e27679, (2011) The aim of the present study was to investigate TLR2 expression in peripheral blood monocytes from dogs naturally infected with Leishmania (Leishmania) infantum to determine whether it correlates with... |
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Heat shock protein 70 regulates platelet integrin activation, granule secretion and aggregation.
Am. J. Physiol. Cell Physiol. 310 , C568-75, (2016) Molecular chaperones that support protein quality control, including heat shock protein 70 (Hsp70), participate in diverse aspects of cellular and physiological function. Recent studies have reported ... |
| MKT-077 |