7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level[1].
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity[1][2].
Apoptosis inducer 9 induces apoptosis with IC50 value of 4.21 μM. Apoptosis inducer 9 induces apoptosis through the mitochondrial pathway and enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Apoptosis inducer 9 can be used the potential to develop new anti-proliferative agents[1].
Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].
HDAC3/6-IN-2 (compound 15) is a potent HDAC6 and HDAC3 inhibitor, with IC50 values of 0.368 and 0.635 μM, respectively. HDAC3/6-IN-2 shows antitumor activity, and induces cancer cell apoptosis. HDAC3/6-IN-2 decreases the levels of HDAC6 and HDAC3, associated with upregulation of acetylated H3 and α-tubulin[1].
Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research[1].
Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis[1][2].
Pipermethystine is an alkaloid that can be isolated from the Kava plant. Pipermethystine decreases HepG2 cell cellular ATP levels, mitochondrial membrane potential, and induces apoptosis[1].
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages[1][2].
Etidronic acid (Etidronate) disodium is an orally and intravenously active bisphosphonate. Etidronic acid disodium inhibits resorption of bone, reduces arterial calcification and can be used for osteoporosis research. Etidronic acid disodium has anticancer activity. Etidronic acid disodium is a chelating agent and can be used to remove heavy metal in water[1][2][3][4].
Quercetin is a natural flavonoid which activates or inhibits the activities of a number of proteins. Quercetin can activate SIRT1 and inhibit PI3K with IC50s of 2.4 μM, 3.0 μM, 5.4 μM for PI3K γ, PI3K δ and PI3K β, respecti
Bim BH3 is a biological active peptide. (This Bim peptide belongs to the pro-apoptotic Bcl-2 family of proteins.)
Vallesiachotamine, a known monoterpene indole alkaloid, possesses anti-tumor activity[1].
AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions[1][2].
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma[1][2].
Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis[1].
Taraxerol is isolated from Abroma augusta L, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis[1][2].
L-Glutathione reduced-13C2,15N (GSH-13C2,15N) is the 13C- and 15N-labeled L-Glutathione reduced. L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
Mcl1-IN-1 is an inhibitor of myeloid cell factor 1 (Mcl-1) (IC50=2.4 µM).
Lithocholic acid-d4 (3α-Hydroxy-5β-cholanic acid-d4) is the deuterium labeled Lithocholic acid, which is a toxic secondary bile acid[1].
Metoprolol-d5 is the deuterium labeled Metoprolol[1]. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[2][3][4].
PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
Echitamine chloride is the major monoterpene indole alkaloid present in Alstonia with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 µM[1][2].
PSB 0474 (3-phenacyl-UDP) is a selective and potent P2Y6 receptor agonist with an EC50 of 70 nM[1]. PSB 0474 inhibits cell proliferation, increases NO release in astrocytes and microglia cells. PSB 0474 induces astrocytes apoptosis[2].
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research[1].
Anticancer agent 102 is a derivative of tetracaine. Anticancer agent 102 has anti-cancer activity. Anticancer agent 102 induces apoptosis[1].
Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research[1].
3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects[1][2].
C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity. C25-140 expands studying the impact of the ubiquitin system on immune signaling and underscores the importance of TRAF6 E3 ligase activity in psoriasis and rheumatoid arthritis (RA)[1].