kras degrader-1

KRAS degrader-1 (compound 1) is a potent agent that selectively targets KRAS proteins for degradation via the autophagy-lysosomal pathway [1].

Pan-KRAS degrader 1 (Compound 1) is a broad-spectrum KRAS degrader, exhibiting an inhibitory constant Ki value of 25 nM against KRASG12V as determined by surface plasmon resonance (SPR). Additionally, this compound demonstrates antitumor activity.

PROTAC KRAS G12C degrader-1, a cereblon-based degrader, promotes CRBN KRAS G12C dimerization and facilitates the degradation of GFP-KRAS G12C in reporter cells [1].

PROTAC K-Ras Degrader-1 is a PROTAC degrader based on the Cereblon E3 ligand, capable of degrading K-Ras.

PROTAC K-Ras Degrader-3 is a PROTAC degrader targeting K-Ras, exhibiting a DC50 value of ≤ 1 nM against SW620 KRAS G12D and a GI50 value of ≤ 10 nM in inhibiting the growth of SW620 3D cells. It is used in cancer research.

Pan-KRAS Ligand 1 serves as a ligand for the target protein of PROTAC (Ligand for Target Protein for PROTAC). This compound facilitates the synthesis of PROTAC Pan-KRAS Degrader 4.

PROTAC SOS1 degrader-1, a potent compound, demonstrates an effective degradation of PROTAC SOS1 with a DC50 value of 98.4 nM. It exhibits antiproliferative activity against cancer cells harboring diverse KRAS mutations and has shown an antitumor effect with low toxicity [1].

TUS-007, a modified CANDDY (Chemical knockdown with Affinity aNd Degradation DYnamics) molecule originally derived from a proteasome inhibitor, scarcely affects proteasome activity. It is a potent, orally active degrader of KRAS G12D V, effective in cell-free chemical knockdown of KRAS G12D V. Furthermore, TUS-007 has been shown to suppress tumor growth [1].

PROTAC KRAS G12C Degrader-3 (Comp 283) serves as a potent degrader of KRAS G12C, utilized in cancer research [1].

PROTAC KRAS G12C degrader-2 (compound 432) acts as a bifunctional modulator, enhancing the hydrolysis of K-Ras protein. One end of this compound features a cereblon inhibitor of apoptosis proteins (IAP), while the other end contains a moiety that binds to KRAS [1].