mcf-7

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

γ-Tocotrienol (Plastochromanol) is one of the four types of tocotrienol, a type of vitamin E. Itl is also a radioprotector, antioxidant. It shows antitumor and antihypertensive effects in vivo.

Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.

(Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.

1. Octyl Gallate is an antioxidant approved by the US Food and Drug Administration (FDA) as a food additive. 2. Octyl Gallate has antimetastatic activity. 3. Octyl Gallate shows antimicrobial activity against H. pylori, with a minimum inhibitory concentration (MIC) value of 125 ug/mL. 4. Combination therapy with octyl gallate and ferulic acid improves cognition and neurodegeneration in a transgenic mouse model of Alzheimer's disease.5. Octyl Gallate is a potential anticancer agent, it exhibited decreased MCF-7 & MDA-MB-231 survival and induced apoptosis, with IC50 value of 40 uM. 6. Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) has antiviral activity, it shows an inhibitory effect on the growth of herpes simplex virus type 1 (HSV-1) in HEp-2 or Vero cells. 7. Octyl gallate shows antifungal activity against Saccharomyces cerevisiae ATCC7754 and Zygosaccharomyces bailii ATCC 60483.

Genistin (Genistoside) is the major isoflavonoid of soybeans and soy products.It has been reported to possess various therapeutic effects, including anti-inflammatory and anticancer activities

EB1 is a potent and selective MNK kinase inhibitor with inhibitory effects on MNK1 and MNK2 with IC50 values of 0.69 μM and 9.4 μM, respectively.EB1 inhibits the growth of cancer cells, promotes apoptosis, and inhibits the phosphorylation of eIF4E.

4-Methoxycinnamyl alcohol showed toxicity to MCF-7, HeLa and DU145 cancer cell lines with IC50 values of 14.24, 7.82 and 22.10 μg/mL, respectively. 4-Methoxycinnamyl alcohol was isolated from Foeniculum vulgare. 4-Methoxycinnamyl alcohol did not show apoptotic effects but showed necrosis after 48 h in a 10 μg/mL DNA fragmentation study.

Tubulin inhibitor 24 is a potent inhibitor that can inhibit tubulin polymerization.

Alisol F 24-acetate is a natural product isolated from Alisma plantago-aquatica Linn[1]. Alisol F 24 Acetate enhances chemosensitivity and apoptosis of MCF-7/DOX Cells by inhibiting P-Glycoprotein-Mediated drug efflux[2].

VEGFR2-IN-1 is a selective and potent VEGFR2 inhibitor with antitumor activity that inhibits cell proliferation and migration and can be used in the study of breast cancer.

Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent inhibitor of steroid sulfatase (STS). Estrone O-sulfamate is a placental microsomal inhibitor (P.M.) with IC50 values of 18 nM. Estrone O-sulfamate showed inhibitory effects on STS in MCF-7 cells with IC50 values of 0.83 nM. Estrone O-sulfamate can be used to study cancer.

P-gb-IN-1 is a potent P-glycoprotein (P-gp) inhibitor that exhibits reverse activity by inhibiting P-gp outflow. P-gb-IN-1 has been shown to inhibit P-gp by hydrogen bonding with residues Asn 721 and Met 986. P-gb-IN-1 showed low toxicity in MCF-7/ADR cells.

ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells and potently and selectively inhibits the growth of MCF-7 breast cancer cells (GI50: 0.56 μM).

GLL398 is an oral selective estrogen receptor down-regulating agent that strongly binds to ERα (IC50 =1.14 nM) and effectively degrades ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM).

Ellipticine (Elliptisine) is a potent antineoplastic agent exhibiting multiple mechanisms of action, IC50 of 0.67±0.06, 1.25±0.13, 1.25±0.13, 0.67±0.06, 0.27±0.02, 0.49±0.04, 0.44±0.03, and 1.48±0.62 μM for Leukemia HL-60, Breast adenocarcinoma MCF-7, Breast adenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32, Neuroblastoma UKF-NB-4, Neuroblastoma UKF-NB-3, and Glioblastoma U87 mg cell, respectively.

MTOB (α-keto-γ-Methylthiobutyric acid) is a substrate for c-terminal binding protein (CtBP) that interferes with the carcinogenic activity of CtBP in cell culture and mice. It also actively regulates TCF-4 signaling, leading to cancer stem cell (CSC) growth and self-renewal.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

HS-1793, a resveratrol analogue, downregulates the expression of hypoxia-induced HIF-1 and VEGF and inhibits tumor growth of human breast cancer cells in a nude mouse xenograft model

Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2/Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.

1. Morusin (Mulberrochromene) possesses antitumor effects of cell lines including HT-29, A549, MCF-7, and MDA-MB-231, through suppressing STAT3 and NFκB attenuation mediated apoptosis induction. 2. Morusin possesses anti-oxidant and anti-inflammatory effects.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, shows antinociceptive, anti-inflammatory, and antioxidant activity in various research models.

Idarubicin hydrochloride (Zavedos), a hydrochloride salt form of Idarubicin, is a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells ( IC50: 3.3 ng/mL).

Cedrelone is a citrulline analog and a phenazine biosynthesis-like domain protein (PBLD) activator.Cedrelone induces apoptosis in cancer cells.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone has insecticidal activity, inhibiting the growth of arrowhead venom of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus). Cedrelone has insecticidal activity, inhibiting the growth of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus).Cedrelone has antitumor effects and exhibits significant cytotoxicity against cancer cell lines such as -60, SMMC-7721, A-549, MCF-7, and SW480.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone is a very potent inducer of apoptosis, leading to cell cycle arrest.

Helichrysetin has mild anti-HIV-1 PR activity. Helichrysetin has great potentials for development as an anticancer agent, it has cytotoxic effect on four selected cancer cell lines, A549, MCF-7, Ca Ski, and HT-29.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

Parthenosin (Quercetin 3-O-β-D-glucuronide butyl ester), a flavonoid derived from the aerial parts of Calligoum polygonoides, exhibits cytotoxic properties with IC50 values of 60.46 μg/mL for HepG2 and 61.4 μg/mL for MCF-7 cell lines [1].

Peganumine A, a natural product isolated from Peganum harmala, exhibits cytotoxic activity with IC50 values of 5.8 µM for HL-60 cells, 38.5 µM for MCF-7 cells, 40.2 µM for PC-3 cells, and 55.4 µM for HepG2 cells [1].

Antiproliferative Agent-39 (Compound 12) effectively inhibits the proliferation of various cancer cell lines, including A549, SNU-638, Col2, HT1080, and MCF-7, with respective IC50 values of 11, 25, 14, 11, and 6.3 μM [1].

Araliadiol is a polyacetylenic compound isolated from the leaves of Aralia cordata Thunb. Araliadiol inhibits MCF-7 cell growth (IC50: 6.41 µg/mL).

2α,3α,24-Trihydroxyurs-12-en-28-oic acid, a triterpenoid phytoalexin, shows antifungal activity against the fungus mentioned. It also shows in vitro cytotoxic activity against tumor cell lines including PLC,Hep3B,HepG2,HeLa,SW480,MCF-7 and Bel7402.

Dodecanoic acid ingenol ester, a natural compound, shows moderate cytotoxicity with IC50 values being 35.59 μM (Caco-2), 24.04 μM (MCF-7), and 22.24 μM (MCF-7/ADM).

FAK-IN-7 has potential antiproliferative activity and is a FAK inhibitor.

Camellianin A is a flavonoid series of compounds derived from A. nitida and tea that exhibits anticancer activity, inhibits angiotensin-converting enzyme (ACE) activity, and promotes apoptosis in Hep G2 and MCF-7 cells.Camellianin A prevents CCl4-induced liver injury by exerting anti-oxidative stress, anti-inflammatory, and anti-apoptotic properties.

Necrocide 1 (compound (S)-38), a potent anticancer agent, exhibits antiproliferative activity with IC50 values of 0.48 nM for MCF-7 and 2 nM for PC3 cancer cell lines, respectively [1].

Ru3 is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor that prompts apoptosis in MCF-7 cells through various mechanisms, including DNA damage induction, inhibition of DNA repair, alteration of cell cycle distribution, reduction of mitochondrial membrane potential, and elevation of intracellular reactive oxygen species (ROS) levels [1].

Protoapigenone, an antineoplastic agent extracted from ferns, demonstrates notable inhibitory activity against various cancer cell lines, including Hep G2, Hep 3B, MCF-7, A549, and MDAMB-231. The respective IC50 values are 1.60, 0.23, 0.78, 3.88, and 0.27 μg/mL [1].

Cyclo(Gly-His) is a cyclic dipeptide encompassed within liposomes, exhibiting antimicrobial and anticancer properties with cytotoxic effects on HeLa and MCF-7 cells, demonstrating IC50 values of 1.699 mM and 0.358 mM, respectively. This compound is relevant for drug delivery system research [1].

CDK2-IN-20 (compound 3b), a CDK2 inhibitor, exhibits cytotoxic effects on tumor cells with an IC50 ranging from 5.52-17.09 µM. It arrests the MCF-7 cell cycle at the S phase and induces apoptosis [1].

Anticancer Agent 149 (compound 3), isolated from the rhizome of Dioscorea dioscorea (DM), demonstrates selective cytotoxicity against MCF-7 cells with an IC50 of 31.41 μM [1].

Anticancer agent 33 (compound 3), derived from Squamocin and Bullatacin, exhibits potent inhibitory activity against the 4T1 breast cancer cell line (A549, HeLa, HepG2, and MCF-7 cells), with IC50 values ranging from 1.9 to 5.4 µM [1].

5,7-Dimethoxy-2,3-phenanthrenediol exhibits estrogenic activity by promoting the proliferation of MCF-7 cells and enhancing the expression of ERβ within this cell line [1].

YL-109, a novel anticancer agent, can inhibit breast Y cell growth and invasiveness in vitro and in vivo.

Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermentation, extraction, purification and physico-chemical and biological propertiesJ Antibiot. (Tokyo)33(7)683-689(1980) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

Diallyl tetrasulfide is an organosulfur compound that has been found in A. sativum and has diverse biological activities, including antimicrobial, antioxidant, and anticancer properties.[1],[2],[3],[4] It is active against the bacteria S. aureus and methicillin-resistant S. aureus (MRSA; MICs = 0.5 and 2 mg/L, respectively), as well as the fungi C. albicans, C. krusei, C. glabrata, A. niger, A. flavus, and A. fumigatus (MICs = 0.5, 4, 2, 1, 2, and 4 mg/L, respectively).[1] It reduces cadmium-induced increases in hepatic levels of thiobarbituric acid reactive substances (TBARS) and increases cadmium-induced decreases in the hepatic activity of superoxide dismutase (SOD1), catalase, GST, and glucose-6-phosphate dehydrogenase (G6PDH) in rats when administered at a dose of 40 mg/kg.[2] Diallyl tetrasulfide is cytotoxic to MCF-7 breast cancer cells (IC50 = 92 μM) and reduces tumor growth in a BGC-823 mouse xenograft model when administered at doses of 20, 30, and 40 mg/kg for 32 days.[3],[4]

Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) is an inducer of ferroptosis.1 It induces ferroptosis, but not apoptosis or necroptosis, in NB1 cancer cells when used at a concentration of 3 μM.1 Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) inhibits proliferation of BJAB, NALM-6, Jurkat, MelHO, and MCF-7 cancer cells (IC50s = 0.07, 2.5, 1.5, 3, and 5 μM, respectively), as well as NALM-6 cells resistant to daunorubicin and vincristine when used at concentrations ranging from 0.04 to 0.125 μM.2 |1. Sagasser, J., Ma, B., Baecker, D., et al. A new approach in cancer treatment: Discovery of chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) complexes as ferroptosis inducers. J. Med. Chem. 62(17), 8053-8061 (2019).|2. Lee, S.-Y., Hille, A., Kitanovic, I., et al. [FeIII(salophene)Cl], a potent iron salophene complex overcomes multiple drug resistance in lymphoma and leukemia cells. Leuk. Res. 35(3), 387-393 (2011).

7-Isopentenyloxy-gamma-fagarine has highly cytotoxicity against the MCF-7and Jurkat cell line. It has been used as a precursor for the chemical asymmetric synthesis of the enantiopure alkaloids: evoxine, anhydroevoxine and evodine.

Glochidonol exhibits strong inhibitory effects against three human tumor cell lines, MCF-7, NCI-H-460 and SF-268, the GI(50) values of 9.0 +/- 3.7, 4.9 +/- 0.2 and 9.8 +/- 0.5, respectively; it also exerts its antiproliferative activity through the involv