breast cancer cell death

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.

SI-2 is an inhibitor (SMI) of steroid receptor coactivator-3 (SRC-3 or AIB1). SI-2 can selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells, and selectively induce breast cancer cell death with IC50 values in the low nanomolar range (3-20 nM), but not affect normal cell viability.

HJ-PI01 (HJ-PI01) is a Pim-2 inhibitor. HJ-PI01 (HJ-PI01) induces apoptosis and autophagic cell death in triple-negative human breast cancer.

OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea

Larotaxel (XRP9881) is a taxane analogue with anticancer activity that promotes tubulin assembly and stabilizes microtubules, inducing apoptosis. It crosses the blood-brain barrier and has a higher affinity for Docetaxel than P-glycoprotein 1, making it useful for studying breast and bladder cancer.

ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.

LXG6403 is a powerful dual-thiazole LOX cell activity inhibitor with an IC50 of 1.3 μM. It exhibits anticancer properties by restructuring the extracellular matrix, enhancing the penetration of chemotherapeutic drugs, inducing reactive oxygen species (ROS) production, and promoting cell death mediated by DNA damage, thereby overcoming chemotherapy resistance in triple-negative breast cancer.

ERK1/2 inhibitor 10 (Compound 36c) is a potent inhibitor of ERK1 and ERK2, with IC50 values of 0.11 nM and 0.08 nM, respectively. It effectively hinders the phosphorylation of downstream substrates p90RSK and c-Myc. Additionally, ERK1/2 inhibitor 10 induces apoptosis and incomplete autophagy-related cell death. This compound demonstrates significant antitumor efficacy in models of triple-negative breast cancer and colorectal cancer harboring BRAF and RAS mutations.

F3-PEG8-RiboTAC is a RiboTAC compound that specifically degrades the mRNA of the oncogene LGALS1. This compound can induce apoptosis (cell death) in tumor cells and inhibit their invasion. F3-PEG8-RiboTAC exhibits antitumor activity and is applicable in research on leukemia and triple-negative breast cancer. (RNase L ligand; RNA binder; Linker)

TNI-97 is a selective, orally active HDAC6 inhibitor with an IC50 value of 0.2 nM. It significantly suppresses the growth and colony-forming abilities of the triple-negative breast cancer (TNBC) cell line MDA-MB-453. In these cells, TNI-97 induces widespread cell death, including apoptosis, necroptosis, and pyroptosis. Additionally, TNI-97 demonstrates antitumor activity in mouse models bearing MDA-MB-453 xenograft tumors or syngeneic mouse-derived TNBC cell allograft tumors. TNI-97 is useful for researching triple-negative breast cancer.

Ferroptosisinducer-8 is a ferroptosis (iron-dependent cell death) inducer with high selectivity against other cell death pathways. It induces ferroptosis by affecting ACSL4, GPX4, and FTH1, disrupting intracellular iron homeostasis and the GSH/GPX4 antioxidant defense system, leading to the accumulation of lipid peroxides. Ferroptosisinducer-8 also stimulates ROS production and can inhibit tumor growth, making it useful for research in triple-negative breast cancer (TNBC).

Apoptosis inducer41 is an apoptosis-inducing agent that prompts cell death through the mitochondrial pathway. It exhibits significant inhibitory effects on MCF-7 cells, with an IC50 of 6.2 μM. Apoptosis inducer41 notably arrests MCF-7 cells in the G2/M phase, increases the accumulation of reactive oxygen species (ROS), and induces mitochondrial membrane potential depolarization. This compound is applicable in breast cancer research.

Tingenin B is a potent anticancer agent due to its cytotoxic activity on cancer stem cells of breast cancer in vitro. Tingenin b was cytotoxic against MCF-7s (IC50: 2.38 μM for 48 h) by inducing apoptosis. Endoplasmic reticulum stress was also found to be

Collismycin A is a bacterial metabolite from *Streptomyces* with antibacterial, antiproliferative, and neuroprotective properties. It exhibits activity against various bacteria (MICs = 6.25-100 μg/ml) and fungi (MICs = 12.5-100 μg/ml). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s = 0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50 = 56.6 μM) but not MDA-MD-231 breast cancer cells (IC50 > 100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) in a 2:1 ratio, with iron ions inhibiting its antiproliferative effect on HeLa cells, an effect not observed with zinc, manganese, copper, or magnesium ions. Additionally, Collismycin A (1 μM) reduces apoptosis in zebrafish larvae brain regions by 44% in a model of neuronal cell death induced by all-trans retinoic acid.

DMBA (7,12-Dimethylbenz[a]anthracene) is a carcinogenic polycyclic aromatic hydrocarbon (PAH) that can be used to induce animal models of leukemia, liver cancer, breast cancer, skin cancer, and lung cancer. It is also capable of inducing programmed cell death (apoptosis) in A20.1 murine B-cell lymphoma.

Chevalone C is a meroterpenoid fungal metabolite originally isolated from E. chevalieri. It is active against M. tuberculosis H37Ra (MIC = 6.3 μg/ml) and is cytotoxic to BC1 human breast cancer cells (IC50 = 8.7 μg/ml). Chevalone C inhibits the growth of multidrug-resistant isolates of E. coli, S. aureus, and E. faecium in a disc diffusion assay when used at a concentration of 15 μg/disc. It also induces cell death in HCT116 colorectal carcinoma cells.

BRD4/CK2-IN-1 is a small molecule inhibitor targeting BRD4 and CK2, with an IC50 of 180nM for BRD4 and 230nM for CK2. It inhibits the proliferation of MDA-MB-231 and MDA-MB-468 cells, inducing apoptosis and autophagy-related cell death. It can be used in triple-negative breast cancer research.

Eupatorin has antiproliferative and antiangiogenic effects. Eupatorin has antiproliferative and cytostatic effects on MDA-MB-468 human breast cancer cells due to CYP1-mediated metabolism. Eupatorin-induced cell death is mediated by both the extrinsic and

VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2)/M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma.

NSC243928 mesylate binds to human lymphocyte antigen 6 (LY6), a cell growth inhibitor with anticancer activity, and induces cell death in triple-negative breast cancer cells in a LY6K-dependent manner.

OTS193320, an imidazopyridine compound, acts as an inhibitor of SUV39H2 methyltransferase activity. It effectively reduces global histone H3 lysine 9 tri-methylation levels in breast cancer cells, promoting apoptotic cell death. When combined with Doxorubicin (DOX), OTS193320 enhances the reduction of γ-H2AX levels and decreases cancer cell viability more significantly than when either agent is used alone.

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.

Indium (III) thiosemicarbazone 5b is an anticancer compound demonstrating cytotoxicity against various cancer cell lines including A549, MCF-7 breast, cisplatin-resistant MCF-7/DDP breast, and Hl 7702 liver cancer cells, with IC50 values of 2.41, 1.97, 2.11, and 8.95 µM, respectively. It effectively lowers PI3K, Akt, mTOR, P-gp, and GSH levels in MCF-7/DDP cells. In vivo studies show that at a dosage of 2.5 µmol/kg, indium (III) thiosemicarbazone 5b significantly reduces tumor weight and volume in MCF-7/DDP mouse xenograft models. Furthermore, liposomes formulated with this compound promote apoptosis and pro-death autophagy in MCF-7/DDP cells, alongside notable reductions in tumor volume and weight, showcasing its potential as a therapeutic agent in cancer treatment.

AD-8007, an acetyl CoA synthase 2 (ACSS2) inhibitor, can cross the blood-brain barrier and significantly reduces lipid storage and cell colony formation in vitro models while increasing tumor cell death. With its anti-cancer activity, AD-8007 is useful in breast cancer research [1].