PROTAC KSP degrader 1

PROTAC KSP degrader 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 degrader 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 degrader 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) )

Product Specifications

CAS Number

[3099825-86-9]

UNSPSC

12352211

Target

Apoptosis; Kinesin; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-ksp-in-1.html

Smiles

O=C(NCCCCCCCCNC(COC1=C2C(C(N(C3CCC(NC3=O)=O)C2=O)=O)=CC=C1)=O)[C@@H](N)CSC4(C5=CC=C(OC)C=C5)C6=CC=CC=C6C=CC7=C4C=CC=C7

Molecular Formula

C48H51N5O8S

Molecular Weight

858.01

References & Citations

[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.