a2780 cells

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Carboplatin (JM-8) is a cisplatin derivative, a DNA synthesis inhibitor. Carboplatin binds to DNA, inhibits replication and transcription, and induces cell death. Carboplatin has antitumor activity.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

Thymohydroquinone (Thymoquinol) is a monoterpenoid phenolic compound found in thyme, oregano, and other plants in the labiaceae family. Thymohydroquinone inhibits cancer cell growth, reduces oxidative stress and modulates inflammatory responses, scoured 2, 2-diphenyl-1-PicrylHydrazyl radicals in a cell-free assay (IC50 = 2.4 μg/ml), In the oxygen radical absorption capacity (ORAC) test at concentrations of 1.6 to 6.4 μg/ml, Its Trolox value was 2.6. Thymus hydroquinone inhibited the growth of A2780, OVCAR-8 and CIS-A2780 ovarian cancer cells (IC50 were 3.1, 8.9 and 9.8 μM, respectively) and human ovarian immortalized epithelial cells (IC50 = 14 μM). It also inhibited Plasmodium falciparum in vitro (IC50 = 15.9 μM).

Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity.

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

GEM144 is a dual inhibitor of DNA polymerase α (POLA1) and HDAC 11. GEM144 induces p53 acetylation, activates p21, arrests the cell cycle in the G1/S phase, and induces apoptosis.

meso-Dihydroguaiaretic acid is a natural lignan exhibiting multiple biological activities, including the inhibition of proliferation in ACC375, COS, and HeLa cells.

2-Methylcyclohexa-2,5-diene-1,4-dione exhibits inhibitory activity against cancer cells such as A2780, HT-29, HL-60, and K562 (IC50 = 2.8–12.1 µM) and antibacterial activity against Bacillus subtilis.

P-gp inhibitor 27 (Compound D2) is an inhibitor of P-glycoprotein (P-gp) that reduces the expression of P-gp and MRP1. It increases the accumulation of Rh123 in A2780/T cells and reverses multidrug resistance to Paclitaxel (EC50 of 88 nM) and Cisplatin.

DS-103 is an HDAC inhibitor that targets HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC50 values of 0.029, 0.123, 0.022, 0.367, and 9.26 μM, respectively. It also inhibits the malignant malaria parasite [Plasmodium falciparum 3D7] with an IC50 of 5.08 μM. In A2780 and Cal27 cells, DS-103 exhibits cytotoxicity with IC50 values of 1.48 μM and 1.47 μM, respectively, and reverses cisplatin resistance in these cells with IC50 values of 4.62 μM and 2.23 μM. DS-103 acts synergistically with cisplatin, enhancing apoptosis induced by cisplatin.

PROTACNAMPT Degrader-1 is an effective NAMPT-targeting PROTAC with a DC50 value of 217 nM. It exhibits antiproliferative activity, with an IC50 value of 0.12 μM against A2780 cells.

E/Z-FETPY is an organic diiron (I) complex with significant cytotoxicity in cancer cell lines, capable of inducing ferroptosis in poorly differentiated cell lines, such as A2780 cells.

Tubulin polymerization-IN-66 (Compound 13) inhibits colony formation and tubulin polymerization while also inducing apoptosis. It reduces cell viability in A549, A2780, SKOV3, and HCC827 cells, with IC50 values of 0.84, 0.38, 0.31, and 0.34 nM, respectively. Additionally, Tubulin polymerization-IN-66 is effective against the Paclitaxel-resistant A2780/T cancer cell line as well as its parent cell line, A2780.

MerTK-IN-2 (compound 15f) is an orally active inhibitor of MerTK with an IC50 of 37.5 nM. It can induce apoptosis and exhibits antitumor activity with IC50 values of 1.79 μM for human ovarian cancer cells (A2780), 18.32 μM for breast cancer cells (MDA-MB-231), and 2.18 μM for colon cancer cells (HCT116).