cancer-initiating

PTC-209 is a potent and selective BMI-1 inhibitor.

YHO-13351 is an ABCG2 inhibitor, an acrylonitrile derivative, that induces sensitization of cancer stem initiating-like side population cells to irinotecan.GSK1702934A can be used to study diabetes.

Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2 M phase. Darinaparsin decreases transcription of Gli-2, a transcription factor that mediates Sonic hedgehog signaling, when used at a concentration of 1.5 but not 3 µM. It decreases SHP1 phosphatase activity and increases ERK phosphorylation. [2] Darinaparsin reduces tumor growth in DU145 and PC3 prostate cancer mouse xenograft models when administered at a dose of 100 mg kg every other day.[1]

Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.

Roy-Bz is a potent and selective activator of protein kinase C delta (PKCδ). It effectively inhibits proliferation in colon cancer cells by initiating a mitochondrial apoptotic pathway that relies on PKCδ and involves the activation of caspase-3.

PTC-209 hydrobromide (PTC-209 HBr) is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).

Fac-[Re(CO)3(L3)(H2O)][NO3] (Compound 3), a rhenium(I) tricarbonyl aqua complex, acts as an anticancer agent through the induction of mitochondrial dysfunction. It exhibits cytotoxicity against prostate cancer cells, demonstrating an IC50 value of 0.32 μM in PC-3 cells. This compound predominantly localizes to the mitochondria, reducing ATP production and triggering paraptosis in PC3 cells, while not initiating necrosis, apoptosis, or autophagy [1].

Nε-(1-Carboxymethyl)-L-lysine (CML), an advanced glycation end product (AGE), is formed through the oxidative modification of glycated proteins under conditions of oxidative stress.1,2,3 Its levels escalate with age, diabetes, cancer, vascular diseases, and various pathologies associated with oxidative stress.1,4,5 CML interacts with the membrane-bound receptor for AGEs (RAGE), initiating signaling via MAPKs and NF-κB pathways. Conversely, a truncated version of RAGE generates a soluble protein that sequesters CML, thereby diminishing this signaling.6,7

NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1 CDK1 levels, leading to G2 M cell cycle arrest and initiating apoptosis through caspase-9 caspase-3 cleavage.