| Identification | Back Directory | [Name]
MKT 077 | [CAS]
147366-41-4 | [Synonyms]
FJ 776
MKT 077
MKT077;MKT-077;FJ-776
MKT-077 >=98% (HPLC), powder
1-Ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-pyridinium chloride
Pyridinium, 1-ethyl-2-[[3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-, chloride (1:1) | [Molecular Formula]
C21H22ClN3OS2 | [MDL Number]
MFCD27665468 | [MOL File]
147366-41-4.mol | [Molecular Weight]
432.002 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
H2O: soluble10mg/mL, clear | [form ]
powder | [color ]
orange to red | [Water Solubility ]
H2O: 10mg/mL, clear | [InChI]
1S/C21H22N3OS2.ClH/c1-4-23-13-9-8-10-15(23)14-18-24(5-2)20(25)19(27-18)21-22(3)16-11-6-7-12-17(16)26-21;/h6-14H,4-5H2,1-3H3;1H/q+1;/p-1/b21-19+; | [InChIKey]
VSKYOTRJSLYFHX-UXJRWBAGSA-M | [SMILES]
CN(C1=C(S/2)C=CC=C1)C2=C3C(N(CC)/C(S\3)=C/C4=[N+](CC)C=CC=C4)=O.[Cl-] |
| Hazard Information | Back Directory | [Description]
MKT-077 is a cationic rhodacyanine dye that demonstrates antiproliferative activity against cancer cell lines (EC50s = 1.4-2.2 μM in vitro) through its ability to inhibit members of the heat shock protein 70 (Hsp70) family of molecular chaperones. It has been shown to bind to an allosteric site conserved in Hsp70 family members, interfering with ATP hydrolysis and abrogating the interaction of the chaperone with the tumor suppressor p53. | [Uses]
MKT-077 is used in the treatment of Alzheimer’s diseases and other tauopathie’s. Also, is a rhodacyanine derivative that selectively targets cancer cells and overcomes tamoxifen resistance | [Biochem/physiol Actions]
MKT-077 is an inhibitor of mitochondrial hsp70 family member, mortalin (mot-2)n; causes selective death of cancer cells. | [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]. | [IC 50]
HSP70 | [storage]
Store at -20°C | [References]
[1] XIAOKAI LI. Analogues of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, As Anti-Cancer Agents[J]. ACS Medicinal Chemistry Letters, 2013, 4 11: 1042-1047. DOI: 10.1021/ml400204n
[2] AIKATERINI ROUSAKI . Allosteric Drugs: The Interaction of Antitumor Compound MKT-077 with Human Hsp70 Chaperones[J]. Journal of Molecular Biology, 2011, 411 3: Pages 614-632. DOI: 10.1016/j.jmb.2011.06.003
[3] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras. |
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| Company Name: |
China Langchem Inc.
|
| Telephone: |
0086-21-58956006 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList19141/0_EN.htm |
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
|