ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors MKT 077

MKT 077

Product NameMKT 077
CAS147366-41-4
MFC21H22N3OS2.Cl
MW432
EINECS
MOL File147366-41-4.mol

Chemical Properties

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-]

Safety Information

WGK Germany	3
RTECS	UU4023332
Storage Class	11 - Combustible Solids
Toxicity	LD50 intraperitoneal in mouse: 50mg/kg

Usage And Synthesis

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 +4°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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