Bioactivity | PROTAC KSP-IN-1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP-IN-1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP-IN-1 exhibits antitumor efficacy in mouse model[1]. (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727)) |
Formula | C48H51N5O8S |
Molar Mass | 858.01 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhao DG, et al., Discovery of novel KSP-targeting PROTACs with potent antitumor effects in vitro and in vivo. Eur J Med Chem. 2025 Jan 15;282:117052. |