COTI-2 (COTI2) is an orally available thiosemicarbazone that may act on mutant forms of p53 and PI3K/AKT/mTOR pathway; induces apoptosis in a wide variety of human tumor cells in culture (IC50s<40 nM), inhibits the proliferation of colorectal cancer cell lines more effectively than cetuximab and erlotinib; shows superior activity against tumor, and is safe and well-tolerated in vivo.
Phase 1 Clinical
HL001 (HL 001) is a potent cyclophilin A (CypA) inhibitor with IC50 of 31.6 nM, induces NSCLC cell cycle arrest and apoptosis via restoring p53 expression; stabilizes p53 through inhibiting the MDM2-mediated p53 ubiquitination, and downregulates G3BP1 and induces ROS and DNA damage; selectively suppresses tumor growth in p53 wild-type NSCLC harboring p53-72R through disrupting interaction between MDM2 and p53-72R in a CypA-dependent manner; synergistically enhance tumor regression in orthotopic NSCLC mouse model combined with cisplatin.
DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity; binds to, and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53; restores p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.
HDM-201 (NVP-HDM 201, Siremadlin) is a highly potent p53-MDM2 interaction inhibitor with biochemical IC50 of 0.13 nM, cellular IC50 of 90 nM; a second generation p53-MDM2 inhibitor that recently entered phase I clinical trial.
NSC-319726 (NSC319726) is an allele-specific p53 mutant reactivator; restores WT structure and function to the p53(R175) mutant; kills p53(R172H) knockin mice with extensive apoptosis and inhibits xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner.
SAR-405838(MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM; activates wild-type p53 in vitro and causes p53-dependent cell-cycle arrest and/or apoptosis; shows durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer, and HCT-116 colon cancer; orally bioactive.
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