tnbc

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-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-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].

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

PU-WS13 hydrobromide is a GRP94 inhibitor with anti-inflammatory activity and inhibits the proliferation of M2-like macrophages in mouse TNBC tumors.

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

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.

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.

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

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

Chrysosplenol D, an efflux pump inhibitor that can potentiate the activity of commercially important antibiotics and antimalarials.

TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A PP2A p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.

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

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.

Rasarfin inhibits Ras and ARF6.

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

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.

Iniparib (BSI-201) (BSI-201) , a PARP1 inhibitor, exhibits potency in triple-negative breast Y (TNBC).

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).

DK-1-150 is an inducer of apoptotic cell death in TNBC cell lines without causing cytotoxicity in the normal mammary epithelial cell line.

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.

PARP-1 2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1 2 and CDK12 with IC50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair and inducing cell cycle arrest and apoptosis. This compound also hampers the proliferation of TNBC cells and the growth of TNBC xenograft tumors [1].

ZMF-23, a PAK1/HDAC6 dual inhibitor, suppresses PAK1 and HDAC6-mediated aerobic glycolysis and cellular migration while inducing TNF-α-regulated necroptosis and augmenting apoptosis. The compound effectively hampers the Warburg effect and cell motility, positioning it as a potential research tool for triple-negative breast cancer (TNBC) [1].

BRD4 CK2-IN-1 is the first potent, orally active dual-target inhibitor of BRD4 CK2 (bromodomain-containing protein 4 casein kinase 2), with inhibitory concentrations (IC50) of 180 nM for BRD4 and 230 nM for CK2. In triple-negative breast cancer (TNBC), BRD4 CK2-IN-1 induces apoptosis and autophagy-related cell death.

LL-K8-22 is a potent, selective, and durable dual degrader of CDK8-cyclin C, demonstrating DC50 values of 2.52 and 2.64 μM, respectively. This compound effectively suppresses STAT1 Ser 727 phosphorylation and inhibits carcinogenic transcriptional programs driven by E2F and MYC. LL-K8-22 is specifically utilized in research for triple-negative breast cancer (TNBC) [1].

Glembatumumab vedotin (CDX-011) is an antibody-drug conjugate with potent anticancer effects, utilized in the study of triple negative breast cancer (TNBC).

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

Anticancer agent 57 (compound 14) demonstrates potent inhibition of MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50 values ranging from 6.43 to 8.00 μM. Additionally, this agent induces cell cycle arrest and promotes apoptosis. In vivo studies using nude mice xenografted with MADMB-231 cells have shown that Anticancer agent 57 effectively inhibits tumor growth. Consequently, Anticancer agent 57 can serve as a valuable tool for researching triple negative breast cancer (TNBC) [1].

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

TS-24 is an inhibitor of the cysteine protease histatin S (CTSS).TS-24 promotes BRCA1-mediated apoptosis and shows radiosensitization in a TNBC xenograft mouse model.

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

G4/HDAC-IN-1, a dual-targeting compound for G4 and HDAC, shows inhibition of intracellular HDAC activity, with an IC50 value of 1.1 μM, and promotes G4 formation. It effectively inhibits proliferation and tumor growth in a TNBC xenograft model, presenting potential for cancer research applications.

MS8815, a selective proteolysis targeting chimera (PROTAC) degrader of enhancer of zeste homolog 2 (EZH2), exhibits inhibitory activity with an IC50 value of 8.6 nM. It is utilized in the research of triple-negative breast cancer (TNBC) [1].

Escin IA (Escin IA;Aescin IA) is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].

mTOR/HDAC6-IN-1 is an effective dual inhibitor of histone deacetylase (HDAC6) and mammalian rapamycin (mTOR). The IC50 values for HDAC6 and mTOR are 56 nM and 133.7 nM respectively. MTOR/HDAC6-IN-1 can significantly induce autophagy and apoptosis and inhibit migration. MTOR/HDAC6-IN-1 has potential in the study of triple negative breast cancer (TNBC).

GPX4-IN-6 is a small molecule covalent GPX4 inhibitor (IC50: 0.12 μM) with antitumour activity.GPX4-IN-6 induces ferroptosis and is used for the treatment= and prevention of triple negative breast cancer (TNBC).

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

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

BJ-2302 is a SRC inhibitor. BJ-2302 effectively suppressed MDA-MB-231 cell invasion (Matrigel invasion assay) and metastasis (chorioallantoic membrane assay xenografted with MDA-MB-231-luc2-tdTomato cancer cells). Additionally, BJ-2302 (1 mg/kg) strongly suppressed TNBC cell proliferation in vitro and tumor growth in a xenograft mouse tumor model. The anti-metastatic and anti-tumor effects of BJ-2302 were superior to those of Z-FL-COCHO (1 mg/kg) or batimastat (30 mg/kg), a pan-MMP inhibitor.

DK-1-166 is a inducer of apoptotic cell death in TNBC cell lines without causing cytotoxicity in the normal mammary epithelial cell line.

SHP2 CDK4-IN-1 (compound 10) is a dual inhibitor targeting SHP2 and CDK4, with oral activity and high potency, showing IC50 values of 4.3 nM for SHP2 and 18.2 nM for CDK4. It induces G0 G1 arrest, inhibits proliferation of TNBC cell lines, and demonstrates significant antitumor efficacy in the EMT6 syngeneic mouse model. This compound is valuable for research into triple-negative breast cancer (TNBC) [1].

JMX0293, an O-alkylamino-tethered salicylamide derivative, demonstrates strong efficacy against the TNBC MDA-MB-231 cell line with an IC50 of 3.38 μM, while showing minimal toxicity towards the non-tumorigenic human breast epithelial cell line MCF-10A, where its IC50 exceeds 60 μM. It inhibits STAT3 phosphorylation, contributing to apoptosis in MDA-MB-231 cells, and significantly suppresses MDA-MB-231 xenograft tumor growth in vivo, all without notable toxicity.

JG-231 is a JG-98 analog with anticancer activity.JG-231 inhibits the MDA-MB-231 xenograft tumor model of triple-negative breast cancer (TNBC).JG-231 inhibits the interaction of Hsp70-BAG3.JG-231 inhibits the MDA-MB-231 xenograft tumor model of triple-negative breast cancer (TNBC). JG-231 inhibits MDA-MB-231 xenograft tumor model of triple negative breast cancer (TNBC).

2',3'-Dehydrosalannol possesses antifeedant activity against Spodptera litura. It shows anticancer effects on triple-negative breast cancer(TNBC), it inhibits cathepsin-mediated pro-survival signaling which resulted in growth arrest of TNBC cells.

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 hydrochloride, a powerful activator of UNC-51-like kinase 1 (ULK1) with an EC50 value of 18.94 nM, has significant implications in the study of triple-negative breast cancer (TNBC).

PARP1 BRD4-IN-2 is a potent and selective inhibitor of PARP1 (IC50: 197 nM) and BRD4 (IC50: 238 nM), which inhibits DNA damage repair, blocks the G0 G1 cell cycle transition, and induces apoptosis. PARP1 BRD4-IN-2 exhibits antitumor effects in the MDA-MB-468 mouse xenograft tumor model and is used to study triple-negative breast cancer (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.