tnbc

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

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.

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

(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-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.

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.

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).

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.

TMU 35435 is an inhibitor of histone deacetylases (HDAC). It enhances radiosensitivity by inducing the accumulation of misfolded proteins and autophagy (autophagy) in TNBC, and inhibits the NHEJ pathway through ubiquitination of the catalytic subunit of DNA-dependent protein kinase (DNA-PKcs).

Imipramine (Dimipressin) is an orally active Fascin1 inhibitor with antidepressant and antitumor activity.Imipramine inhibits the 5-hydroxytryptamine transporter (IC50: 32 nM), induces apoptosis, and induces autophagy in U-87MG glioma cells.Imipramine has neuroprotective and immunomodulatory activities, inhibits TNT, and is used to label brain blood vessels.Imipramine is a neuroprotective and immunomodulatory compound. Imipramine has neuroprotective and immunomodulatory activities, inhibits invasion and migration of TNBC cells, and can be used to study breast cancer and epilepsy.

YF438 is an HDAC inhibitor that demonstrates potent anti-cancer activity both in vitro and in vivo. It inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and MDM2, inducing the dissociation of MDM2 from MDMX, and promoting the degradation of MDM2.

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.