For research use only, not for therapeutic use.
K858（Cat No.:I004714）is a small-molecule inhibitor targeting the kinesin spindle protein (KSP), which plays a crucial role in mitotic spindle formation during cell division. By inhibiting KSP, K858 prevents the proper assembly of the mitotic spindle, leading to cell cycle arrest and apoptosis, particularly in rapidly dividing cancer cells. This mechanism makes K858 a promising candidate for anti-cancer therapies, especially in tumors resistant to traditional chemotherapeutic agents. Its selective action on KSP reduces the likelihood of off-target effects, offering a targeted approach to cancer treatment with fewer systemic side effects.
| Catalog Number | I004714 |
| CAS Number | 72926-24-0 |
| Synonyms | (R)-N-(4-acetyl-5-methyl-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl)acetamide |
| Molecular Formula | C₁₃H₁₅N₃O₂S |
| Purity | ≥95% |
| Target | ATPase |
| Solubility | 10 mM in DMSO |
| Storage | Store at +4C |
| IC50 | 1.3 μM |
| IUPAC Name | N-(4-acetyl-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide |
| InChI | InChI=1S/C13H15N3O2S/c1-9(17)14-12-15-16(10(2)18)13(3,19-12)11-7-5-4-6-8-11/h4-8H,1-3H3,(H,14,15,17) |
| InChIKey | JEFVYQYZCAVNTP-UHFFFAOYSA-N |
| SMILES | CC(=O)NC1=NN(C(S1)(C)C2=CC=CC=C2)C(=O)C |
| Reference | </br>1:The kinesin Eg5 inhibitor K858 induces apoptosis but also survivin-related chemoresistance in breast cancer cells. De Iuliis F, Taglieri L, Salerno G, Giuffrida A, Milana B, Giantulli S, Carradori S, Silvestri I, Scarpa S.Invest New Drugs. 2016 Aug;34(4):399-406. doi: 10.1007/s10637-016-0345-8. Epub 2016 Mar 19. PMID: 26994617 </br>2:K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells. Nakai R, Iida S, Takahashi T, Tsujita T, Okamoto S, Takada C, Akasaka K, Ichikawa S, Ishida H, Kusaka H, Akinaga S, Murakata C, Honda S, Nitta M, Saya H, Yamashita Y.Cancer Res. 2009 May 1;69(9):3901-9. doi: 10.1158/0008-5472.CAN-08-4373. Epub 2009 Apr 7. PMID: 19351824 Free Article |
