mcf7 cells

WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

PAIB-SOs-12 is an anti-mitotic compound that shows anti-proliferative activity at low concentrations and induces cytoskeletal damage in MCF7 cells.

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions,reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

Rhosin hydrochloride is a specific inhibitor of the RhoA subfamily Rho GTPases and inhibits the RhoA-GEF interaction. Rhosin hydrochloride can significantly induce cell apoptosis without affecting cell cycle progression. [1]

Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7 DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

DPP-21 is an inhibitor of microtubule protein polymerization (IC50: 2.4 μM). It exhibits antiproliferative activity against various cancer cell lines, with IC50 values of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23), and 9.37 nM (HepG2). DPP-21 induces cell cycle arrest at the G2 M phase of mitosis and subsequently triggers apoptosis in tumor cells by decreasing Bcl-2 while increasing pro-apoptotic protein Bax levels.

LLC1, a derivative of amiloride, exhibits cytotoxicity against breast cancer cells, particularly those resistant to other treatments. The compound demonstrates varied IC50 values across several breast cancer cell lines, including 13 mM for MCF7, 12 mM for MCF7 MX-100, 25 mM for MCF7 TS, 26 mM for MCF7 TR-1, and 19 mM for MCF7 TR-5. LLC1 holds potential for research in cancer therapy.

Erα-IN-1 (compound 3c) is an inhibitor of the estrogen receptor α (ERα), effectively blocking ERα activity in MCF7 ERE-LUC cells.

PROTACERα Degrader-10 (Compound 160a) is an orally bioavailable ERα degrader with a DC50 of 0.37-1.1 nM in MCF7, T47D, and CAMA-1 cells. It demonstrates antitumor activity in mouse models.

HL22 is a derivative of harmine. It exhibits significant inhibitory effects on three cancer cell lines: HCT116, MGC803, and MCF7. Moreover, HL22 can impede the migration and colony formation of MGC803 cells. Its anticancer mechanism is associated with multiple metabolic pathways and can be utilized for tumor research.

VEGFR-2-IN-63 (Compound 12b) is an inhibitor of VEGFR2, reducing 87.2% of VEGFR-2 activity at 10 μM. It exhibits anti-proliferative activity against various cancer cells, with IC50 values of 6.5 μM for HCT116, 2.1 μM for MCF7, and 4.1 μM for PaCa2.

SRSF1-IN-1 (STP2) is an inhibitor of SRSF1 that modulates the splicing of Bcl-x precursor mRNA by downregulating SRSF1 expression. It exhibits antitumor activity in vitro and in vivo, with IC50 values ranging from 0.33 to 6.93 μM against cancer cells such as HepG2 and MCF7. In mice, SRSF1-IN-1 demonstrates a high safety profile, as intraperitoneal administration of 1 g kg does not lead to mortality or pathological damage. SRSF1-IN-1 holds potential for research in the field of antitumor therapy [1].

5-HT1AR 5-HT6R ligand-1 (Compound PP13) functions as a ligand for the 5-HT receptor, demonstrating high affinity for 5-HT1AR, 5-HT6R, and 5-HT7R with Ki values of 19, 69, and 198 nM, respectively. In HEK293 cells, it inhibits cAMP production with EC50 values of 1535, 488, and 53 nM for these receptors. Additionally, 5-HT1AR 5-HT6R ligand-1 exhibits antiproliferative effects on several cancer cell lines, including 1321N1, U87MG, MCF7, and AsPC-1, with IC50 values of 9.6, 13.6, 19.3, and 14.6 μM, respectively. The compound also shows antagonistic activity towards the dopamine receptor D2R, with a Ki of 1903 nM.

Estrogen receptor modulator13 (Compound 5D) is an estrogen receptor antagonist with significant cytotoxic effects on MCF7 cells, exhibiting an IC50 value of 8.50 μM. Estrogen receptor modulator13 holds potential for breast cancer research.

BMS-265246 is a potent and selective CDK1 2 inhibitor. Its chemical name is (4-[R-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1H-indol-1-yl]-1H-pyrazolo[3,4-d] pyrimidine-6-amine), and it functions by targeting CDK1 and CDK2 to potentially disrupt cell cycle progression.

Erysolin is a natural product with anti-cancer potential. It is cytotoxic to a variety of cancer cells (DU145, HCT 116, MCF7, HEP3B, SKOV3, SF-268) and has antibacterial activity against Escherichia coli.

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

PIN1 inhibitor 2 (compound 12) is a potent inhibitor of PIN1, demonstrating significant antitumor activity with an IC50 of 9.55 μM against MCF7 cells, making it a promising candidate for breast cancer research [1].

Colletotrichalactones A is a polyketide with moderate-to-potent cytotoxic activity against MCF7 cells, exhibiting an IC50 value of 35.06 μM [1].

(1S,3R)-GNE-502 (compound 179) is a potent ERα degradation agent with an EC50 of 13 nM in MCF7 HCS cells, suitable for studying estrogen receptor-related cancers.

PRMT4-IN-1 is a selective inhibitor of PRMT4, demonstrating an IC50 value of 3.2 nM, and has been shown to reduce the relative viability of MCF7 cells [1].

AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.