mx-1

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1 2 (Kis: 1.2 0.85 nM).

DMX-129 is a chemical compound acting as an inhibitor for both ΙΚΚε and TBK-1, demonstrating efficacy with IC50 values of below 30 nM for each [1].

Rucaparib (PF-01367338) is a PARP protein inhibitor (PARP-1 Ki=1.4 nM) and hexose hexose-6-phosphate dehydrogenase (H6PD) inhibitor with oral activity. Rucaparib exhibits antitumor activity, with activity against desmoplasia-resistant prostate cancer (CRPC).

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood-brain barrier permeable microtubule-disrupting agent with potent and broad-spectrum cytotoxic activities and significant anticancer efficacy in human MX-1 breast cancer and various mouse xenograft cancer models.

Rucaparib Phosphate (PF-01367338 phosphate) is an inhibitor of PARP (Ki: 1.4 nM for PARP1) that is used in clinical therapy to sensitize cancer cells to chemotherapy.

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

S-72 acts as a microtubule polymerization inhibitor, effective in cell-free assays at concentrations of 1, 3, and 10 µM. At nanomolar levels (IC50s = 15.64 and 26.32 nM, respectively), it diminishes the viability of both MCF-7 and paclitaxel-resistant MCF-7/T breast cancer cells. Moreover, at 50 nM, S-72 impedes migration, invasion, and wound healing in these cell lines. Additionally, at 100 nM, it arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7/T cells, while also inhibiting stimulator of interferon genes (STING) activation. In vivo, S-72 dosage at 15 mg/kg per day curtails tumor growth in mouse xenograft models of paclitaxel-resistant breast cancer, specifically MCF-7/T and MX-1/T.

Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7 DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.

Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

LXY6090 is a HIF-1 inhibitor. LXY6090 inhibited the activity of HIF-1 and downregulated the protein level of HIF-1α in breast cancer cells. LXY6090 showed in vivo anticancer efficacy by decreasing the HIF-1α expression in nude mice bearing MX-1 tumor xeno

LLC1, a derivative of amiloride, exhibits cytotoxicity against breast cancer cells, particularly those resistant to other treatments. The compound demonstrates varied IC50 values across several breast cancer cell lines, including 13 mM for MCF7, 12 mM for MCF7 MX-100, 25 mM for MCF7 TS, 26 mM for MCF7 TR-1, and 19 mM for MCF7 TR-5. LLC1 holds potential for research in cancer therapy.

Naproxen is a COX-1 and COX-2 inhibitor (IC50s: 8.72 and 5.15 μM, respectively in cell assay). Naproxen etemesil is a lipophilic and non-acidic prodrug of naproxen. It is hydrolyzed to pharmacologically active Naproxen once absorbed.

(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is an orally active inhibitor of PARP1 2, with Ki values of 1.2 nM and 0.87 nM, respectively. It inhibits cellular PARylation at an EC50 of 2.51 nM. This compound leads to the accumulation of DNA damage and suppresses the proliferation of BRCA1 2-mutated MX-1 and Capan-1 cells, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib exhibits antitumor activity in mouse models.