mcf7 cells

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]

Antitumor agent-87 is a potent compound exhibiting high antitumoral activity, with a Ki value of 0.23 µM for CYP1A1. It demonstrates antiproliferative effects and induces cell cycle arrest at the G2 M phase, underscoring its effectiveness as an antitumor agent.

PSB-15160 is a compound that inhibits the growth of MCF7 (breast), NCI-H460 (lung) and SF-268 (NCS) cells in the treatment of estrogen-dependent tumours.

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

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.

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.

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.

Sangivamycin (NSC-65346) is an effective inhibitor of protein kinase C (PKC, Ki = 10 μM). Sangivamycin exhibits antiproliferative activity against a variety of human cancers.

Isopteleine shows weak cytotoxic activities against human breast cancer cells (MCF7).

cis-Moschamine exerts antitumour effects on HeLa, MCF7 and A431 cells.

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.

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.

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].

PROTAC ERα Degrader-8 (compound ii-56), a highly potent degrader of Erα, achieves a DC50 of just 0.000006 μM in MCF7 cells [1].

PhpC is an analog of G-clamp that exhibits antiproliferative activity against MCF7 cells, with an IC50 of 387.9 μM. It modulates the structure of G-quadruplex-RNA in human cells.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1 S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [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.

Lactate Transporter 1 (Compound 1) serves as an active lactate transporter within living cells and exerts cytotoxic effects, exhibiting IC50 values of 3.36 μM in HeLa, 3.27 μM in CAL27, 5.58 μM in MCF7, and 7.66 μM in MCF10A cells. Additionally, an additive effect with Cisplatin has been observed in HeLa cells [1].

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 + - 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 + - 24.62 microM) but is weaker than finasteride (IC50 = 0.38 + - 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7 ADR cells.

MSNBA is a selective and potent inhibitor of fructose transport through GLUT5 and also acts as a probe of the GLUT5 transporter. MSNBA inhibited GLUT5 fructose uptake in MCF7 cells with KI of 3.2±0.4 μM.

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM 15 nM for G9a GLP). UNC0646(UNC 0646) potently blocks G9a GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

PF-06843195 is a selective PI3Kα inhibitor, demonstrating potent activity with an IC50 of 18 nM in Rat1 fibroblasts and Kis for PI3Kα and PI3Kδ less than 0.018 nM and 0.28 nM, respectively, in biochemical kinase assays. It effectively suppresses the PI3K mTOR signaling pathway and exhibits durable antitumor efficacy[1].

HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative activity, exhibiting IC50 values of 3.65 μM in MCF7 breast cancer cells and 2.71 μM in SKBr3 breast cancer cells.

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].

EGFR/CDK2-IN-1, an inhibitor of both EGFR and CDK2, demonstrates effective cytotoxicity towards MCF7 and HepG2 cells, suggesting its potential application in cancer research.

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

EGFR HER2 DHFR-IN-3 (compound 4c) is an efficacious dual inhibitor of EGFR HER2 with IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively, and also inhibits DHFR with an IC50 of 0.193 μM. It induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

23-epi-26-Deoxyactein (27-Deoxyactein) has anti-inflammatory activity, it inhibits nitric oxide production by reducing iNOS expression without affecting activity of the enzyme. It also has anti-cancer activity, it can inhibit growth of the MCF7 human breast cancer cells and induce cell cycle arrest at G1.

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].

(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.

Antimalarial agent 37 (compound 33), a selective Type Ⅱ kinase inhibitor, exhibits antiplasmodial activity and demonstrates cytotoxicity towards HepG2 and MCF 7 cancer cells [1].

Anticanceragent 242 (7) exhibits anticancer activity across various cancer cell types. For instance, in ovarian adenocarcinoma cells A2780, it shows an IC50 of 0.24 μM and in A2780cis cells, an IC50 of 0.45 μM. Additionally, it demonstrates efficacy in CCD18Co non-malignant human fibroblasts with an IC50 of 0.59 μM, lung adenocarcinoma A549 cells with an IC50 of 0.32 μM, colorectal adenocarcinoma HT29 cells with an IC50 of 0.26 μM, and in breast adenocarcinoma MCF7 cells with an IC50 of 0.55 μM.