tnbc

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).

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.

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.

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

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-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.

Anti-TNBC agent-3 (compound 3g) is a compound that induces apoptosis and possesses anti-cancer cell proliferation properties. It effectively inhibits tumor growth and metastasis in xenograft models of triple-negative breast cancer (TNBC) [1].

Anti-TNBC agent-2 (3j), a purine derivative, acts as an anti-triple negative breast cancer (TNBC) therapeutic. It promotes apoptosis in MDA-MB-231 cells, while also inhibiting their migration and angiogenesis. Moreover, anti-TNBC agent-2 suppresses tumor growth and metastasis, and downregulates Ki67 and CD31 protein expression in TNBC xenograft models. It may be utilized for TNBC research [1].

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.

THZ2 (CDK7-IN-1), an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).

SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13(CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM), which disables triple-negative breast cancer (TNBC) cells

PF-06647263 (anti-EFNA4-ADC) is an ADC compound targeting EFNA4, with anti-tumor activity, composed of an anti-EFNA4 antibody conjugated with calicheamicin, inducing significant tumor regression in TNBC xenografts.

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.

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.

SKLB646 is an orally active multitarget kinase inhibitor that exhibits potent suppression of several kinases. It demonstrates significant inhibitory effects on SRC and VEGFR2, with IC50 values of 0.002 μmol L and 0.012 μmol L, respectively. Additionally, SKLB646 shows notable inhibition of B-Raf and C-Raf, with IC50 values of 0.022 μmol L and 0.019 μmol L, respectively. The compound inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinases. Furthermore, SKLB646 inhibits the proliferation, migration, and invasion of human umbilical vein endothelial cells (HUVEC), thereby suppressing tumor-induced angiogenesis. SKLB646 also displays significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines.