TMV-IN-5 (compound 1a) is an anti-plant virus/fungal agent. TMV-IN-5 inhibits viral assembly by binding to tobacco mosaic virus (TMV) CP. TMV-IN-5 can be used in the development of pesticides[1].
(-)-Sesamin isolated from Asarum forbesii Maxim, is an isomer of Sesamin. Sesamin is a potent and selective delta 5 desaturase inhibitor in polyunsaturated fatty acid biosynthesis[1][2].
SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.IC50 value: 31 nMTarget: PRMT3in vitro: SGC707 is the first PRMT3 chemical probe. SGC707 is a potent PRMT3 inhibitor (IC50=31±2 nM, KD=53±2 nM) with outstanding selectivity (selective against 31 other methyltransferases and more than 250 non-epigenetic targets). SGC707 can engage PRMT3 and effectively inhibit its catalytic activity in cells and that overexpressed PRMT3 can methylate histone H4 in cells. SGC707 stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM in PRMT3 InCELL Hunter Assays.in vivo: SGC707 is bioavailable and suitable for animal studies. This well characterized chemical probe is an excellent tool to further study the role of PRMT3 in health and disease. We assessed in vivo pharmacokinetic (PK) properties of SGC707. Intraperitoneal injection of SGC707 at 30 mg/kg gave good plasma exposure in CD-1 male mice over 6 h with the peak plasma level of 38000 nM. The plasma level of SGC707 at 6 h post injection was 208 nM, more than 2-fold higher than its IC50 value in the cellular assay and the half-life of SGC707 was about 1 h. This mdose was well tolerated by the test animals. These results suggest that SGC707 is suitable for animal studies in addition to cell-based studies.
VP-4556 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4556 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 8 µg/mL. VP-4556 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%[1].
Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect[1].
Ala-Ala-Ala-Tyr-Gly-Gly-Phe-Met
Verrucosin (Compound 3) is a compound isolated from Myristica fragrans[1].
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively[1].
RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research[1].
cis-Nerolidol is a sesquiterpene alcohol that can be found in various plants. cis-Nerolidol exhibits antioxidant and antibacterial activities. cis-Nerolidol can also potentiate the action of antibiotics[1].
eIF4A3-IN-16 (compound 60) is a silvestrol (HY-13251) analogue. eIF4A3-IN-16 interferes the assembling of eIF4F translation complex with EC50s of 1, 30 and 1 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-16 can be used for the research of human cancer pathogenesis[1].
Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties[1].
GV-150013 is a selective CCK-B receptor antagonist. GV-150013 has sleep aid effect[1].
Octylbenzene-d22 is the deuterium labeled Octylbenzene[1].
Tyrphostin AG 1433 is a specific and potent inhibitor of PDGFR-β and of KDR/Flk-1. Tyrphostin AG 1433 acts as an angiogenesis inhibitor[1].
Flutamide-d7 is deuterium labeled Flutamide.
Licoflavone B is a flavonoid isolated from Glycyrrhiza inflata, inhibits S. mansoni ATPase (IC50, 23.78 µM) and ADPase (IC50, 31.50 µM) activity. Anti-schistosomiasis activity[1].
(2S)-N3-IsoSer is a click chemistry reagent, a chiral alpha-hydroxypropinoic acid, containing azide group.
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity[1][2]. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM)[2].
Meptyldinocap (2,4-DNOPC) is a novel powdery mildew (Erysiphe necator) fungicide which shows protectant and post-infective activities.
3-Methylchromone is an active compound which can be used in the prevention and research of anginose attacks of coronary origin[1].
GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.IC50 value: 5.9 nM/6.4 nM(biochemical/cellular assay) [1]Target: BTKin vitro: GDC-0834 inhibited BTK with an in vitro IC(50) of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC(50) of 1.1 and 5.6 μM in mouse and rat, respectively [1].in vivo: Administration of GDC-0834 (30-100 mg/kg) in a rat collagen-induced arthritis (CIA) model resulted in a dose-dependent decrease of ankle swelling and reduction of morphologic pathology [1]. GDC-0834 exhibited low clearance in PXB chimeric mice with humanized liver. Uncertainty in human pharmacokinetic prediction and high interest in a BTK inhibitor for clinical evaluation prompted an investigational new drug strategy, in which GDC-0834 was rapidly advanced to a single-dose human clinical trial. GDC-0834 plasma concentrations in humans were below the limit of quantitation (<1 ng/ml) in most samples from the cohorts dosed orally at 35 and 105 mg [2].
Di-n-dodecyl Phthalate-3,4,5,6-d4 is the deuterium labeled Di-n-dodecyl Phthalate[1].
Amyloid β-Protein (5-42) is aAβ Fragment.
Casein kinase 1δ-IN-5 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 47 nM. Casein kinase 1δ-IN-5 shows neuroprotective and anti-inflammatory properties both in vitro. Casein kinase 1δ-IN-5 has the potential for neurodegenerative diseases research.
(S)-3-Amino-1-chloro-5-methylhexan-2-one hydrochloride is a leucine derivative[1].
Toosendanin, a triterpenoid extracted from the bark of fruit of Melia toosendan Sieb et Zucc, possesses analgesic, insecticidal and anti-inflammatory activities[1].
Sialyllacto-N-tetraose b is a sialylated oligosaccharides. Sialyllacto-N-tetraose b naturally occurs in mammal milk[1].
Fmoc-L-Norleucine is a leucine derivative[1].
Desmosterol ester-d6 is deuterium labeled Desmosterol ester.