triple-negative breast cancer (tnbc)

TTK/PLK1-IN-1 (Formula I) is an inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), with IC50 values of 7 nM and 72 nM, respectively. It regulates the spindle assembly checkpoint (SAC) and exhibits antitumor activity against triple-negative breast cancer (TNBC).

Sacituzumab tirumotecan (SKB264) is an antibody-drug conjugate (ADC) targeting TROP2 (trophoblast cell surface antigen 2), capable of releasing the active payload KL610023 within TROP2-positive tumour cells. an effective topoisomerase I inhibitor that induces DNA damage and leads to cell cycle arrest and apoptosis, for use in non-small cell lung cancer (NSCLC) and triple-negative breast cancer (TNBC).

Rasarfin inhibits Ras and ARF6.

FMF-04-159-2 is a potent covalent cell cycle protein-dependent kinase 14 (CDK14) inhibitor with IC₅₀ of 39.6 nM for CDK14 and 256 nM for CDK2.FMF-04-159-2 is able to reduce α-synuclein (α-Syn ) aggregation in neurons and plays a role in Parkinson's disease models, and also inhibits triple-negative breast cancer (TNBC) progression and metastasis by attenuating Wnt/β-catenin signaling.

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7, possessing therapeutic potential in both hematological and solid tumors.

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

SLLN-15 is an orally active, selective, and potent enhancer of autophagy, activating cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC) [1].

BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.

STAT3-IN-35 is a STAT3 inhibitor that binds to the SH2 domain. This compound inhibits the phosphorylation of STAT3 and exhibits antiproliferative activity in triple-negative breast cancer (TNBC) cell lines. Additionally, STAT3-IN-35 has demonstrated toxicity and potent antitumor activity in TNBC xenograft models.

ZMF-24 is an anti-triple-negative breast cancer (TNBC) agent that exhibits IC50 values of 0.22 μM and 0.44 μM against BT-549 and MDA-MB-231 TNBC cell proliferation, respectively. It targets the eukaryotic translation initiation factor 3 subunit D (EIF3D), disrupting TNBC's energy supply by inhibiting glycolysis. Additionally, ZMF-24 induces TNBC cell apoptosis (apoptosis) by stimulating sustained endoplasmic reticulum stress.

W23-1006 is a selective covalent ALKBH5 inhibitor. It binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. The inhibitory activity of W23-1006 is approximately 30 times stronger than that of FTO and 8 times greater than that of ALKBH3. W23-1006 is applicable for research in triple-negative breast cancer (TNBC).

WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).

ROCK HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).

ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with activity against cancer cells. It demonstrates significant inhibitory effects in a triple-negative breast cancer (TNBC) tumor xenograft model, with a tumor growth inhibition (TGI) rate of 96%.

Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.

HSND80 (Compound 1) is an orally active MNK/p70S6K inhibitor, exhibiting a Kd value of 44 nM for MNK1 and 4 nM for MNK2. The residence time of HSND80 on MNK1 and MNK2 is 45 minutes and 58 minutes, respectively. HSND80 effectively inhibits non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppresses the growth of triple-negative breast cancer (TNBC) cells in vitro.

LA-CB1 is a derivative of Abemaciclib that targets CDK4/6 and promotes their degradation via the ubiquitin-proteasome pathway, thereby blocking the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis (Apoptosis). It demonstrates antiproliferative activity against MDA-MB-231 cells with an IC50 of 0.27 µM and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In highly invasive models like triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth, showing robust dose-dependent antitumor activity. This compound can be utilized in breast cancer research.

MY05 selectively targets c-MYC within cells and disrupts the interaction between MYC and MAX. It binds to intracellular c-MYC, modulating its thermal stability, reducing the transcriptional targets of c-MYC, and exhibiting anticancer activity (TNBC, triple-negative breast cancer).

Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.

SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50 values of 38.69, 40.12, and 59.72 nM, respectively. It also serves as an autophagy agonist, influencing mTOR/p70S6K and NCOA4-mediated ferroptosis, potentially mitigating multidrug resistance. SKLB-D18 demonstrates significantly superior efficacy against triple-negative breast cancer (TNBC) in both in vitro and in vivo studies.

EG31 is an EGFR inhibitor that effectively suppresses the proliferation of triple-negative breast cancer (TNBC) cells by inhibiting the EGFR signaling pathway. It demonstrates a GI50 value of 498.90 nM for MDA-MB-231 cells and 740.73 nM for Hs578T cells, while also inducing apoptosis. Additionally, EG31 retains its antiproliferative activity against 5-fluorouracil (5-FU) resistant TNBC cells, with a GI50 of 519.5 nM. EG31 is applicable in research on TNBC resistance.

KIF2C-IN-1 (Compound 7S9) is a selective and potent small molecule inhibitor of KIF2C. It stabilizes the interaction between KIF2C and microtubule proteins, preventing the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel in Paclitaxel-resistant triple-negative breast cancer (TNBC) cells and, when combined with Paclitaxel, significantly reduces tumor growth in mouse models.

BBOX-IN-1 (compound 58) is a potent BBOX inhibitor with an IC50 of 0.02 μM, and it is applicable in research related to triple-negative breast cancer (TNBC).

AKT-IN-27 (4a) is a potential anticancer drug that functions by selectively targeting Akt-driven signaling pathways. It induces apoptosis by activating caspase-3, causing G2/M phase cell cycle arrest, and disrupting mitochondrial membrane potential. AKT-IN-27 (4a) is applicable in research on triple-negative breast cancer (TNBC).