MDM-2/p53 Inhibitor

GY1-22 is an inhibitor of DNAJA1-mutP53^R175H interacting pocket. GY1-22 can be used for the research of cancer.

HIPK2-IN-1 is an orally active and selective HIPK2 inhibitor with an IC₅₀ of 0.56 μM. HIPK2-IN-1 exerts antifibrotic and anti-inflammatory activities. HIPK2-IN-1 binds to HIPK2, inhibits the downstream TGF‑β/Smad3, p53, and TNF‑α/NF‑κB signaling pathways, reduces the expression of fibrotic markers, suppresses cell proliferation and migration, and alleviates renal tubular injury and collagen deposition. HIPK2-IN-1 is used for the study of renal fibrosis associated with chronic kidney disease.

LQFM030 is a novel small molecule MDM2 inhibitor. LQFM030 exhibits concentration dependent cytotoxicity in K562 cells (IC₅₀ = 0.28 mM). LQFM030 induces cell apoptosis through G0/G1 phase cell cycle arrest and increased Caspase activity. LQFM030 downregulates the mRNA expression of MDM2, MDMX, p73, MYC, and NF-κB. LQFM030 is commonly used in research on cancers such as leukemia.

Topoisomerase I/IIα-IN-1 (Compound 20i) is a Topoisomerase I/IIα inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has relatively poor anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma.

cis,trans-Germacrone is an isomer of Germacrone (HY-N0440) and is present in the stems and leaves of Curcuma wenyujin. Germacrone exhibits a wide range of antitumor, antioxidant, and anti-inflammatory effects. Germacrone inhibits lung cancer cell proliferation and alters Akt/MDM2/p53. Germacrone also induces cell cycle arrest at the G1/S phase. Germacrone is used in lung cancer-related research.

AM-8553 is a MDM2/p53 inhibitor (K_D: 0.4 nM for MDM2). AM-8553 has anti-tumor activity

MDM2-IN-27 targets MDM2 protein (K_i = 0.4 nM). MDM2-IN-27 activates the anti-tumor activity of p53 and induces apoptosis by blocking the negative regulation of p53 by MDM2.

Siremadlin (NVP-HDM201) succinate is an MDM2 inhibitor and cell cycle regulator. Siremadlin succinate blocks the p53-binding pocket of MDM2, inhibits MDM2-mediated ubiquitination and degradation of p53, thereby activating the p53 pathway in p53 wild-type cells. Siremadlin succinate can be used in the research of cutaneous melanoma.

ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.

Tubulin polymerization-IN-85 (Compound C21) is a tubulin polymerization inhibitor (IC₅₀ = 1.59 μM) targeting the colchicine binding site. Tubulin polymerization-IN-85 can cause cancer cells G2/M phase arrest and induce apoptosis. Tubulin polymerization-IN-85 downregulates the expression of Bcl-2, Bcl-xl, Mcl-1, Cyclin B1, cdc25, cdc2 protein and upregulates P53, P21, Bad and Bax levels. Tubulin polymerization-IN-85 can be used for the research of cancer, such as cervical cancer.

Antiproliferative agent-8 (Compound 5a) is an anti-cancer agent. Antiproliferative against-8 has antiproliferative activity. Antiproliferative agent-8 significantly increases the P53 levels.

S100A2-p53-IN-1 (compound 51) is a S100A2-p53 interactions inhibitor. S100A2 is a Ca²⁺ binding protein with implications in cell signaling and is known to be upregulated in pancreatic cancer. S100A2-p53-IN-1 can inhibit the growth of the MiaPaCa-2 pancreatic cancer cell line (GI⁵⁰ of 1.2-3.4 μM).

NVP-CFC218 is a selective TP53-MDM2 inhibitor with a structure and biochemical profile similar to NVP-CGM097 (HY-15954) (IC₅₀ of 1.6 nM: displacing the p53 peptide from the surface of HDM2). It is used to analyze pharmacological sensitivity in cell lines and is also applicable in cancer research ^[1] .

OM-301 is a human monoclonal antibody that targets MDM2.

MDM2-IN-27 (Compound 20k) is an MDM2 inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has a certain topoisomerase I inhibitory activity and has a very weak inhibitory effect on topoisomerase IIα. MDM2-IN-27 exhibits significant anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma.

Phage-derived 12/1 peptide exhibits antitumor activity by targeting MDM2 and MDMX, an thus disrupt the MDM2-p53 and MDMX-p53 interaction, with IC₅₀ of 0.15 and 1.25 μM.

pDI is a peptide. pDI inhibits MDM2-p53 and MDMX-p53 interactions with IC₅₀s of 10 and 100 nM respectively. pDI can be used in the research of colorectal cancer.

MI-2103 is a MDM2 inhibitor with an IC₅₀ of 48.1 nM. MI-2103 inhibits the growth of leukemia and breast cancer cells; it exerts no growth-inhibitory effect on cancer cells with p53 mutation or deletion. MI-2103 serves as a target protein ligand for the synthesis of MG-277 (HY-130122). MI-2103 is applicable to the research of leukemia and breast cancer.

MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/ MDM4 inhibitor and p53 activator with the IC₅₀ values of 70.7 nM for MDM2- p53 and 81.4 nM for MDM4-p53 complexes. MDM2/4-p53-IN-2 regulates the cell cycle, induces cell apoptosis and has anticancer activity.

p53-MDM2-IN-2 (Compound 5q) is an orally active p53-MDM2 inhibitor with a K_i value of 0.25 μM. p53-MDM2-IN-2 exerts antitumor activity by inhibiting NF-κB pathway.