mcf-7 cell lines

Indotecan (LMP-400) is an effective inhibitor of topoisomerase 1(Top1) (IC50: 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively).

GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) < 0.1 nM) was observed.

ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).ERD-308 is a highly potent PROTAC degrade

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

4'-Methoxyflavonol is a synthetic flavonol with an additional 3-hydroxyl group and higher antioxidant capacity than 4'-Methoxyflavone.4'-Methoxyflavonol interacts with the lipid bilayer of DPPC model membranes, and is capable of scavenging free radicals and antioxidant activity in DPPH assays, and exhibits some antiproliferative activity against K562 and MCF-7 cancer cell lines.

GSTP1-1 inhibitor 2 (Compound 5g) is an inhibitor of hGSTP1-1 (glutathione S-transferase P1-1), exhibiting an IC50 of 12.2 μM. It demonstrates substantial cytotoxicity against the cell lines DU-145, PC3, and MCF-7, with CC50 values of 36.6, 11.9, and 17.4 μM respectively, making it relevant for research in cancer therapeutics.

YSY01A is a proteasome inhibitor that suppresses cancer cell survival by inducing apoptosis (Apoptosis). It demonstrates IC50 values against various cell lines such as HEK293T, A549, MCF-7, MGC-803, and PC-3M with values of 51.01, 9.21, 5.21, 8.9, and 35.4 nM respectively. Additionally, YSY01A serves as a degrader of gp130 and JAK2, eliminating constitutive STAT3 signaling in human A549 lung cancer cells by downregulating gp130 and JAK2. YSY01A holds potential for research in cancer therapeutics.

Antiproliferative agent-59 (Compound 14u) acts as an inhibitor of tubulin polymerization. Demonstrating anticancer activity in Huh7, SGC-7901, and MCF-7 cell lines, this compound achieves IC50 values of 0.03, 0.18, and 0.13 μM, respectively. Additionally, it arrests the cell cycle at the G2 M phase and induces apoptosis in Huh7 cells. In a xenograft mouse model utilizing Huh7 cells, Antiproliferative agent-59 exhibits antitumor effects against hepatocellular carcinoma without significant toxicity.

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ERα (IC50 = 863 nM). In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote β-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM). The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

Antitumor agent-191 (Compound 7) exhibits antiviral activity against HSV-1 and HIV, with EC50 values of 0.03 μM and 0.81 μM, respectively. It also demonstrates potential antitumor properties by inhibiting cancer cell lines HepG2, WI-38, Vero, and MCF-7, with IC50 values of 19.6, 39.3, 18.3, and 28 μM, respectively.

Aromatase-IN-4 (Compound 6a) is an inhibitor of the enzyme aromatase. It displays anticancer properties, with GI50 values for different cell lines as follows: 2.95 μM for MDAMB-231, 3.35 μM for MCF-7, 2.27 μM for A-549, 8.46 nM for NCI-H23, and 1.56 μM for A-498. Aromatase-IN-4 effectively blocks the estrogen production that depends on aromatase.

Hsp90-IN-39 (Compound 16t) is an HSP90 inhibitor with significant selectivity for the HSP90α isoform. It demonstrates notable antiproliferative activity across various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 is applicable for cancer research.

ERK1 2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.

Anticanceragent 267 (Compound 5q) serves as an activator of RIPK3 and MLKL. It effectively inhibits the proliferation of several cancer cell lines, with IC50 values of 9.79, 10.77, and 5.94 μM for MDA-MB-231, MDA-MB-486, and MCF-7, respectively. The compound induces cell cycle arrest at the subG1 phase and triggers necroptosis in MDA-MB-231 cells. Additionally, Anticanceragent 267 demonstrates antitumor activity in mouse xenograft models.

Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor that binds to the colchicine site on tubulin, causing G2/M cell cycle arrest and inducing reactive oxygen species (ROS) production. It demonstrates significant inhibitory activity against P-glycoprotein (P-gp) overexpressing cell lines MCF7/ADR and KBV200, with resistance indices (DRI) of 0.83 and 0.58, respectively. In an MCF-7 xenograft model, Antitumor agent-200 (at 25 mg/kg, administered intraperitoneally) achieves a 57.2% tumor growth inhibition rate. This compound is applicable for research in the field of cancer therapy.

Metahexestrol is an inhibitor of the estrogen receptor (E2R) with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cell line with an ED50 of 1.0 μM. Additionally, Metahexestrol shows inhibitory activity in estrogen receptor-negative MDA-MB-231 cell lines, and its antiproliferative effect is not reversed by estrogen, suggesting that its mechanism may be partially independent of the E2R pathway. Metahexestrol is applicable in research on estrogen-dependent breast cancer.

Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. It effectively blocks estrogen production and inhibits the proliferation of breast cancer cell lines such as MCF-7, arresting the cell cycle in the G1 phase and inducing apoptosis. Aromatase-IN-5 shows promise for breast cancer research.

PD-M6 is an mTOR PROTAC degrader with a DC50 of 4.8 μM, which facilitates the ubiquitination and degradation of mTOR. It inhibits the proliferation of cancer cell lines HeLa, MCF-7, and HepG2 with IC50 values of 11.3, 2.58, and 3.23 μM, respectively, and induces autophagy. Additionally, PD-M6 specifically targets the degradation of the key protein LAMTOR1 in the mTOR signaling pathway.

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

EGFR-IN-156 (Compound 7f) is an EGFR inhibitor with inhibitory activity against mutant EGFRL858R and EGFRT790M, with IC50 values of 0.186, 0.131, and 0.107 μM, respectively. It exhibits significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer), with IC50 values of 1.67, 5.32, and 6.56 μM, respectively. EGFR-IN-156 suppresses cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. It shows potential in EGFR-related cancers.

Govaniadine is a natural potent inducer of apoptosis in MCF-7 cell lines.

CAY10701 is a 7-deazahypoxanthine analog that prevents microtubule formation, blocking the proliferation of HeLa and MCF-7 cells (GI50s = 22 and 38 nM, respectively). It also inhibits the growth of several different colorectal cancer cell lines (GI50 values range from 9 to 17 nM), while being at least 1,500-fold less effective against normal human fibroblast WI38 cells. CAY10701 is effective in vivo, reducing tumor volume in colorectal cell xenografts in mice without significantly altering body weight.

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of DHA with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple-negative breast cancer cell lines [MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549] at 50-100 μM but increases the proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and dendritic cells with EC50 values of approximately 8-16 μM.