mkn1

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

Eras-4001 is a small-molecule pan-KRAS inhibitor capable of targeting both wild-type KRAS and various mutant forms simultaneously. Eras-4001 inhibits signaling between KRAS and effector proteins such as RAF, thereby blocking the activity of the RAS/MAPK pathway. In preliminary studies, this compound has demonstrated high affinity for KRAS (nano-molar IC₅₀) and induced tumor regression in multiple KRAS-mutant tumor models, indicating potential value for antitumor therapy.

CDK2 degrader7 is an orally active CDK2 degrader with DC50 values of 13 nM in MKN1 cells and 17 nM in TOV21G cells. It induces G1 phase arrest in MKN1 cells and achieves tumor suppression in the HCC1569 (CCNE1 amplified) xenograft model. CDK2 degrader7 is utilized in research on CCNE1 amplification-type cancers.

TTK-IN-5 is an orally active and selective covalent threonine tyrosine kinase (TTK) inhibitor with an IC50 of 8.918 nM. It demonstrates antiproliferative activity against several cell lines, including MDA-MB-231, A2780, HCT116, HCC1569, and MKN1, with IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively. In xenograft mouse models using A2780 and MDA-MB-231, TTK-IN-5 effectively inhibits tumor growth without significant toxicity. TTK-IN-5 is applicable in research on cancers such as breast and ovarian cancer.

CDK2 degrader2 is a PROTAC class CDK2 degrader that targets the CDK2 protein for ubiquitination, facilitating its degradation via the ubiquitin-proteasome pathway (UPP). It effectively degrades CDK2 in MKN1 cells, with a DC50 value of less than 100 nM and an average Dmax greater than 75%.