anticancer effect

BAY 2666605 is an orally active inhibitor of PDE3A (IC50 = 87 nM) and PDE3B (IC50 = 50 nM) with noted anticancer effects.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Trastuzumab deruxtecan (T-DXd) is an antibody-active molecule conjugate (ADC) with anticancer and antitumor activity, which is composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2) coupled to a topoisomerase I inhibitor (DXd). Trastuzumab deruxtecan has an improved effect on the treatment of HER2-positive breast cancer and gastric cancer.

Asperphenamate is a fungal metabolite of Aspergillus flatiipes. The IC50s for T47D cells, MDA-MB-231 cells, and HL-60 cells are 92.3 μM, 96.5 μM, and 97.9 μM. Asperphenamate shows an anticancer effect.

Isomer-Turosteride (Isomer-Turosteride(Isomer-137099-09-3)) is a novel 5 alpha-reductase inhibitor.The antiprostatic effect of Isomer-Turosteride in adult rats is associated with the inhibition of the conversion of T to DHT.Isomer-Turosteride induces a decrease in prostate DHT independent of a secondary increase in T. Isomer-Turosteride has anticancer activity and inhibits the growth of tumor cells. Turosteride has anticancer activity and inhibits the growth of tumor cells. Translated with www.DeepL.com Translator (free version)

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]

Roslin 2 bromide (Benzylhexamethylenetetramine bromide) is a p53 reactivator that disrupts the binding of FAK and p5, exhibiting anticancer effects.

Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.

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.

Cuminaldehyde (Cuminal) is a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity,with a pleasant smell and contributes to the aroma of essential oils.

SR9243, an LXR inverse agonist, can induce LXR-corepressor interaction; shows anticancer activity and selectively targets the lipogenesis and Warburg effect.

Monensin is an antiprotozoal agent produced by Streptomyces cinnamonensis. It has an inhibitory effect on the Wnt β-catenin signaling cascade. Monensin is a prospective anticancer drug for the therapy of neoplasia with deregulated Wnt signaling.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6 JAK2 STAT3 signaling. Icaritin at low concentration (4 or 8 μMol L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.

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. Oxypeucedanin ((+-)-Oxypeucedanin) has novel anticancer effect, mediated via induction of G2-M cell cycle arrest and apoptosis in human prostate carcinoma DU145 cells. 2. Oxypeucedanin is a kind of open-channel blocker of the hKv1.5 channel and it prolongs the APD; therefore, it is an excellent candidate as an antiarrhythmic drug for atrial fibrillation.

TASK-1-IN-1 is a potent and selective inhibitor of TASK-1 (Potassium Channel) with an IC50 of 148 nM, and exhibits a reduced inhibitory effect on the TASK-3 channel with an IC50 of 1750 nM. TASK-1-IN-1 also demonstrates anticancer effects.

Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

MY-875 is a potent microtubulin polymerization inhibitor that competes at colchicine binding sites, exhibiting an IC50 value of 0.92 μM. It effectively suppresses microtubulin polymerization, exerting its inhibitory effect. Additionally, MY-875 exerts its biological impact by activating the Hippo pathway, inducing apoptosis, and displaying commendable anticancer activity [1].

Anticancer agent 54 is an effective anticancer agent whose anticancer activity depends on DNA embedding and ROS generation. Anticancer agent 54 has an anti-proliferative effect by blocking the cell cycle in G0 G1 phase and inducing apoptosis.

K20 is a potent and selective inhibitor of KRas G12C (IC50: 1.16 nM). In H358 cells, K20 demonstrates an anticancer effect with an IC50 value of 0.78 μM and inhibits the growth of NCI-H358 tumor cells (TGI: 41%) without significant toxicity. K20 reduces the phosphorylation level of Erk, leading to apoptosis.

Neogambogic acid, an active ingredient in garcinia, can inhibit the growth of some solid tumors [resulting in an anticancer effect], and may be responsible for the inhibition of proliferation of human breast cancer cell line MCF-7 cells.

TPMP-I-2 has an anticancer effect of immunotoxins.

BCR-ABL-IN-4 is a BCR-ABL inhibitor exhibiting anticancer activity with an inhibitory effect on cancer cell growth, specifically on K562 cells (IC50: 0.67 nM) and BCR-ABL T315I-transfected Ba F3 cells (IC50: 16 nM).