mcf7

Rhosin hydrochloride is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin hydrochloride does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin h

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.

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.

9-dihydro-13-acetylbaccatin III (9-DHAB III)is an apoptosis inducer. It shows cytotoxicity against the MCF7 cell line and drug-resistant cell line MCF7-ADR.

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.

Angeloylgomisin H shows moderate cytotoxic activities with IC50 values ranging from 100 to 200 ug mL against MCF7, HEK293 and CAL27 cell lines.

Oxyphenisatin acetate inhibits the growth of the breast cancer cell lines MCF7, T47D, HS578T, and MDA-MB-468.

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

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.

CADD522 (MFCD00167693) is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM, with antitumor activity

SPP-86 is an effective and selective cell-permeable inhibitor of RET tyrosine kinase with an IC50 of 8 nM.

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.

TMBIM6 antagonist-1 (BAX-inhibitor-1) is a bax inhibitor

LY3405105 (1-Piperidinecarboxylic acid, 4-[[5-methyl-3-(1-methylethyl)pyrazolo[1,5-a]pyrimidin-7-yl]amino]-, 1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-3-pyrrolidinyl ester) is a novel CDK7 inhibitors.

BRD4 Inhibitor-24 is a BRD4 small molecule inhibitor with antitumor activity.

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

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

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.

Tubulin Inhibitor 38 (Compound 14), a tetrazole-based agent, demonstrates significant antiproliferative effects by inducing mitotic arrest and blocking the cell cycle at the G2/M phase, ultimately triggering apoptosis. Administered at 100 nM for 24 hours, it shows considerable cytotoxicity and selectivity within HeLa, MCF7, and U87 MG cell lines [1].

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].

VEGFR-2 DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2 DHFR-IN-2 holds promise for cancer research [1].

VEGFR-2 DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

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].

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.

JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibody blockade prevented cellular retention of JAS239 indicating direct interaction with ChoKα independent of the choline transporters and catabolic choline pathways. In mice bearing orthotopic MCF7 breast xenografts, optical imaging with JAS239 distinguished tumors overexpressing ChoKα from their empty vector counterparts and delineated tumor margins.

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].

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Palazestrant (OP-1250) is an orally available and highly potent estrogen receptor antagonist and selective ER degrader with antitumor activity.Palazestrant inhibits 17b-estradiol (E2), inhibits MCF7 and CAMA-1 cell proliferation, and can be used in breast cancer research.

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.

EGFR HER2 DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively, and exhibits anticancer activity, displaying IC50 values of 9.14, 7.33, 14.18, 24.87, 20.07, and 6.16 μM in Hep G2, HeLa, HEp-2, HCT 116, PC-3, and MCF7 cancer cell lines, respectively; it also reduces the growth of breast cancer tumors [1].

XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.

Aloesin is a C-glycosylated chromone compound found in aloe (Liliaceae) that inhibits tyrosinase (IC50 = 0.9 mM), an enzyme responsible for catalyzing the first step of the conversion of tyrosine to melanin.

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).

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.

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.

EGFR/HER2/TS-IN-1 are EGFR, HER2 and TS (Thymidylate synthase) inhibitors with IC50 values of 0.203, 0.088 and 0.168 μM, respectively, and have the ability to induce apoptosis (MCF7 cell death).

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].

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.

Neohelmanthicin A (compound 3A), a phenylpropanoid with antitumor properties, exhibits IC50 values of 0.13 μM, 7 μM, and 23 μM against leukemia cell line EL4, breast cancer cell line S180, and breast cancer cell line MCF7, respectively [1].

Neohelmanthicin B, a phenylpropanoid isolated from Thapsia garganica, demonstrates cytotoxic properties against EL4, S180, and MCF7 cell lines, with respective IC50 values of 10, 5, and 12 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].

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].

Derrone may be interesting antimicrobial agents to be used against infectious diseases caused by many pathogens. It is also a novel Aurora kinase inhibitor, it can significantly inhibit the formation and growth of MCF7 tumor spheroids.

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.

(-)-Pinocembrin demonstrates anti-mycobacterial activity against Mycobacterium tuberculosis H37Ra, presenting IC 50 values of 1.11 mg/mL in the dormant phase and 1.21 mg/mL in the active phase. Additionally, this compound exhibits significant antiproliferative effects on various cell lines, including THP-1, A549, Panc-1, HeLa, and MCF7, with IC 50 values ranging from 1.88 to 11.00 mg/mL.

NCGC00378430 is a potent SIX1 EYA2 interaction inhibitor that disrupts the [SIX1 EYA2] complex, EMT, and metastasis.

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