Biological Activity
Occupies mortalin-2 (mot-2), a member of the Hsp70 family, at its p53 binding site and enables p53 translocation to the nucleus. Selectively cytotoxic; causes growth arrest of cancer cells in culture. Also inhibits telomerase activity and cross-links F-actin.
Compound Libraries
MKT 077 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 432 |
| Formula | C21H22ClN3OS2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 147366-41-4 |
| PubChem ID | 3037933 |
| InChI Key | VSKYOTRJSLYFHX-UXJRWBAGSA-M |
| Smiles | CN(C1=CC=CC=C1S2)/C2=C4/C(N(CC)/C(S4)=CC3=CC=CC=[N+]3CC)=O.[Cl-] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.6 | 50 | |
| water | 21.6 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 432. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.31 mL | 11.57 mL | 23.15 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.63 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wadhwa et al (2000) Selective toxicity of MKT-077 to cancer cells is mediated by its binding to the hsp70 family protein mot-2 and reactivation of p53 function. Cancer Res. 60 6818 PMID: 11156371
Wadhwa et al (2002) Rhodacyanine dye MKT-077 inhibits in vitro telomerase activity but has no detectable effects on telomerase activity in vivo. Cancer Res. 62 4434 PMID: 12154051
Tikoo et al (1999) Treatment of Ras-induced cancers by the F-actin cappers tensin and chaetoglobosin K, in combination with the caspase-1 inhibitor N1445. Cancer J.Sci.Am. 5 293 PMID: 10526670
Patury et al (2009) Pharmacological targeting of the Hsp70 chaperone. Curr.Top.Med.Chem. 9 1337 PMID: 19860737
Keywords: MKT 077, supplier, MKT077, heat, shock, proteins, 70, Hsp70, Hsps, inhibitors, inhibits, telomerase, inhibitors, inhibits, F-actin, cross-linkers, Hsp70, Hsp70, Tocris Bioscience
