Helvolic acid (Fumigacin) is an antibiotic isolated from Xylaria sp, active against the Gram-positive bacteria[1].
Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia[1][2].
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
Acetylcholine iodide is a common neurotransmitter found in the central and peripheral nerve system[1].
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM，induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM[1].
A potent, and selective Bax agonist (Ki=43.3 nM) that induces conformational changes in Bax by blocking S184 phosphorylation; shows no affinity for other Bcl2 family members, including Bcl2, Bcl-XL, Mcl-1, Bcl-w, Bfl-1/A1, Bid or Bak; facilitates Bax insertion into mitochondrial membranes and forming Bax oligomers, leads to cytochrome c release and apoptosis in human lung cancer cells; potently suppresses lung tumour growth via apoptosis by selectively activating Bax in vivo without significant normal tissue toxicity.
Latinone, a neoflavonoid isolated from Dalbergia cochinchinensis, has antiosteoporotic activity[1].
8-Lavandulylkaempferol is a flavonoid that can be isolated from Sophora flaWescens. 8-Lavandulylkaempferol exhibits cytotoxic activity against the KB epidermoid carcinoma cell line with an IC50 of 15.1 μg/mL[1].
Antimycobacterial agent-4 is a 2-amino-4-(2-pyridyl) thiazole derivative, with antimycobacterial activity, antiplasmodial activity, and cytotoxicity on a mammalian cell line[1][2].
Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress[1][2].
Rosin is isolated from pine wood or pine stumps, Rosin is a frequent contact allergen which induces allergic contact dermatitis[1].
1,3,9-Trimethyluric acid is a natural alkaloid compound[1].
N4-Benzoyl-5’-O-DMTr-2’-O-(N3-trifluoroacetyl) aminopropyl cytidine 3’-CED phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
2,2-Dimethyl-1,3-dioxolane-4-methanol-d5 is the deuterium labeled 2,2-Dimethyl-1,3-dioxolane-4-methanol[1].
Mogroside III, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
7-Hydroxy-5-methoxycoumarin is a phloroglucinol-type furocoumarins, a potent naturally-occurring insect antifeedant[1].
PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib[1].
CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC50 value of 0.031 μM in CHBO subseries and an Ki value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research[1].
3,5-Dicaffeoyl-epi-quinic acid can be extracted from Chrysanthemum morifolium. 3,5-Dicaffeoyl-epi-quinic acid has antioxidant activities. 3,5-Dicaffeoyl-epi-quinic acid can scavenge DPPH radical and superoxide anion radical, with IC50s of 5.6 and 2.9 μg/mL respectively[1].
Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity[1].
Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an IC50s of 28-29 nM[1].
Detajmium (L-tartrate) is an antiarrhythmic compound. Detajmium has effect on V max in both dog ventricular muscle and Purkinje fibers was frequency dependent[1].
Thalidomide-O-amido-C11-COOH (compound IMiD acid 1) is an E3 ligase ligand and linker CRBN (Cereblon) conjugate. Thalidomide-O-amido-C11-COOH can be used to synthesize PROTAC that target the degradation of DOT1L[1].
Sulfanitran is a sulfonamide antiinfective drug.
N-Benzyloleamide is a maccamide isolated from Lepidium meyenii (Maca). N-Benzyloleamide irreversibly inhibits fatty acid amide hydrolase (FAAH). N-benzyloleamide influences the energy metabolism and reveals antioxidant and antifatigue activities[1][2].
Fmoc-Pro-OH is a proline derivative[1].
Cholecystokinin is a peptide hormone. Cholecystokinin, as a hunger suppressant, inhibits food intake and stimulates the digestion of fat and protein. Cholecystokinin can be used for the research of gastrointestinal system[1][2][3].
3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 µM, an Ki value of 0.58 µM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies[1].
Diglycolic acid-d4 is the deuterium labeled Diglycolic acid[1].