sjsa-1

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

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.

BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM). BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft. And it concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.

AM-6761 is a potent inhibitor of the MDM2-p53 interaction. In the SJSA-1 osteosarcoma xenograft model, AM-6761 shows excellent antitumor activity with an ED50 of 11 mg/kg.

MI-1061 TFA, a potent and orally bioavailable MDM2 inhibitor (MDM2-p53 interaction), demonstrates significant chemical stability with an IC 50 of 4.4 nM and a K i of 0.16 nM. It effectively activates p53 and induces apoptosis within SJSA-1 xenograft tumor tissues in mice, showcasing notable anti-tumor activity [1].

Aurora Kinases-IN-4 (Compound 11c) is a covalent, ATP-competitive inhibitor of aurora kinase A with an IC50 value of 1.7 nM. It inhibits cell proliferation in SJSA-1, MDA-MB-231, A549, and HeLa cell lines with IC50 values of 4.27, 1.54, 3.08, and 6.99 μM, respectively. This compound is applicable in research concerning triple-negative breast cancer (TNBC) [1].

(S,R,S)-MI-1061 is an isomer of MI-1061. It serves as a precursor for synthesizing Antibody-Drug Conjugates (ADCs). MI-1061 acts as a potent, orally bioavailable, and chemically stable inhibitor of MDM2 (MDM2-p53 interaction) with IC50=4.4 nM and Ki=0.16 nM. This compound activates p53 and induces apoptosis in murine SJSA-1 xenograft tissues, exhibiting antitumor properties.