tnbc

SBP-7455 potently inhibited ULK1/2 enzymatic activity in vitro and in cells, reduced the viability of TNBC cells and had oral bioavailability in mice.

Rasarfin inhibits Ras and ARF6.

AGX51 is an antagonist of inhibitor of DNA binding (ID) proteins. AGX51 treatment lead to pan-Id degradation, cell cycle arrest, and cell death.

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).

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis.

COTI-2, an orally available thiosemicarbazone, is an activator of mutant forms of the p53 protein with potential antineoplastic activity.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

2-Hydroxychalcone (2-(2-Hydroxybenzal)Acetophenone) can be used as antiparasitic hit compounds when Methoxylated.It can inhibit invasion of triple negative breast cancer cells.

LYN-1604 is a novel ULK1 activator.It inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis.

(6R)-FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect.

YK-3-237 (B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid) reduces acetylation of mtp53 and exhibits anti-proliferative effects toward triple-negative breast cancer (TNBC) cells carrying mtp53.

FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect, inducing a dramatic decrease in cell proliferation and survival in various breast cancer cells.

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.

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.

Anti-TNBC agent-4 (compound 7) exhibits strong inhibitory activity against various TNBC cells, with an IC50 range of 0.37 to 1.52 μM. It inhibits IKKβ-mediated phosphorylation of IκB and p65, and induces apoptosis in TNBC cells.

Anti-TNBC agent-5 (compound 10C) is an inhibitor of triple-negative breast cancer (TNBC) that exhibits favorable stability and pharmacokinetic properties. It demonstrates antiproliferative activity across various cancer cell types. Additionally, in the MDA-MB-231 xenograft model, anti-TNBC agent-5 effectively suppresses TNBC lung metastasis activity. This compound is useful for cancer research.

Anti-TNBC agent-6 (compound pt-3) is an effective agent against triple-negative breast cancer (TNBC). It exhibits cytotoxic activity and induces autophagy (autophagy) and ferroptosis (ferroptosis). Additionally, anti-TNBC agent-6 enhances intracellular ROS accumulation and demonstrates antitumor activity, offering potential for breast cancer research.

anti-TNBC agent-7 (Compound 13c) exhibits anticancer activity and functions as a molecular probe to identify and regulate the signaling of the USP21/JAK2/STAT3 axis. It demonstrates nanomolar cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC).

anti-TNBC agent-1 is a highly effective compound specifically targeting and combating triple-negative breast cancer (TNBC), demonstrating remarkable potency against various breast cancer cell types with IC50 values ranging from 0.20 μM to 0.27 μM. Its mechanism of action involves inducing apoptosis in SUM-159 cells through the mitochondria pathway and causing G1 phase arrest in these cells.

KW-2450 Formate is an IGF-1R/IR tyrosine kinase inhibitor with antitumor effects that acts through inhibition of Aurora A and B kinases.KW-2450 Formate inhibits the growth of TNBC xenografts and induces tetraploid accumulation.