WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205804
Description: 4SC-205 is a small-molecule inhibitor of the human kinesin-related motor protein Eg5 with potential antineoplastic activity. Eg5 kinesin-related motor protein inhibitor 4SC-205 selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and cell death. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein essential for the regulation of spindle dynamics, including assembly and maintenance, during mitosis.
MedKoo Cat#: 205804
4SC-205 is not in stock. This product may be available through custom synthesis when its structure is available.
Synonym: 4SC205; 4SC 205; 4SC-205
IUPAC/Chemical Name: NONE
The following data is based on the product molecular weight Batch specific molecular weights may vary from batch to batch due to the degree 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||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
4SC-205 is an oral small-molecule inhibitor of the human kinesin spindle protein Eg5, which is of crucial importance for proper cell division (mitosis). Mitosis inhibitors, such as taxol, are used as the first-line therapy in numerous cancers. As opposed to taxol, which is neurotoxic, 4SC- 205 does not directly affect microtubules, but only the kinesin Eg5 which is only present during cell division. This compound is in the Phase I AEGIS study in patients with solid tumours or malignant lymphoma in order to evaluate its safety, tolerability, pharmacokinetics and pharmacodynamics. Currently, 4SC-205 is the only oral Eg5 kinesin inhibitor in clinical development. Eg5 interacts with microtubules, a component of the mitosis mechanism, and mediates the segregation of the two spindle poles resulting in the correct distribution of the chromosomes to the daughter cells. Allosteric inhibition of Eg5 by 4SC- 205 leads to cell cycle arrest in mitosis and subsequent programmed cell death (apoptosis). Mitosis is the fundamental process required for cell division and tissue proliferation. The mitotic spindle apparatus has for decades been a primary target for the development of anti-mitotic drugs such as taxanes and vinca alkaloids, which are broadly used in cancer therapies as single chemotherapeutic agents or in combination. In preclinical tests, 4SC-205 has proven to be a particularly efficacious inhibitor of tumour cell proliferation of various cancer origins, both in vitro and in vivo. (source: http://www.4sc.de/product-pipeline/clinical/4SC-205).