n-Butyl-β-D-fructofuranoside could be isolated from kangaisan. n-Butyl-β-D-fructofuranoside induces apoptosis through the mitochondrial pathway. n-Butyl-β-D-fructofuranoside can be used for cancer research[1].
Corynoxine B is an oxindole alkaloid isolated from Uncaria rhynchophylla (Miq.) Jacks (Gouteng in Chinese); a Beclin-1-dependent autophagy inducer. IC50 value:Target: Autophagy inducerin vitro: Corynoxine B, a natural autophagy inducer, restores the deficient cytosolic translocation of HMGB1 and autophagy in cells overexpressing SNCA, which may be attributed to its ability to block SNCA-HMGB1 interaction [1].in vivo: Corynoxine B exhibited prolongation of the thiopental-induced hypnosis on oral administration in mice [2].
1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine-d70 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine. 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE) is a phosphoethanolamine (PE) lipid that can be used in the synthesis
Dihydromunduletone is a rotenoid derivative that selectively inhibits GPR56 (IC50=21 uM) and GPR114/ADGRG5, but not GPR110 or Class A GPCRs; maximally inhibits GPR56 at 50 uM, also dramatically inhibits GPR114 7TM–stimulated Gs activity; also inhibit the growth of the zebrafish intersegmental vessels.
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.
Quinethazone is an orally active diuretic agent and is also a weak inhibitor of carbonic anhydrase. Quinethazone can be used for hypertension research[1][2].
PfGSK3/PfPK6-IN-1 (compound 23e) is a potent inhibitor of plasmodial kinases PfGSK3 and PfPK6, with IC50s of 97 nM and 8 nM, respectively. PfGSK3/PfPK6-IN-1 exerts antiplasmodial activity against blood stage Pf3D7 parasites with an EC50 value of 1.4 mM[1].
Angiotensin II (5-8), human is an endogenous C-terminal fragment of the peptide vasoconstrictor angiotensin II[1]. Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca2+ levels. Angiotensin II also acts at the Na+/H+ exchanger in the proximal tubules of the kidney[2][3].
Lactate (Lactate acid) is the product of glycolysis. Lactate is produced by oxygen lack in contracting skeletal muscle in vivo, and can be removed under fully aerobic conditions. Lactate can be as a hemodynamic marker in the critically ill[1][2].
Tubeimoside I(Lobatoside-H) is an extract from Chinese herbal medicine Bolbostemma paniculatum (MAXIM.) FRANQUET (Cucurbitaceae) has been shown as a potent anti-tumor agent for a variety of human cancers.IC50 value:Target: Anticancer natural compoundin vitro: TBMS I inhibited the proliferation of both HepG2 and L-02 cells in a dose- and time-dependent manner, but HepG2 cells appeared more sensitive to the agent. When exposed to TBMS I for 24, 48 and 72 h, IC50 for HepG2 cells versus L-02 cells were 15.5 vs. 23.1, 11.7 vs. 16.2, 9.2 vs. 13.1 (μM, p<0.01), respectively. TBMS I induced cell shrinkage, nuclear condensation and fragmentation, cell cycle arrest at the G2/M phase, mitochondrial membrane disruption, release of cytochrome c from the mitochondria, activation of caspase 3 and 9, and shifting Bax/Bcl-2 ratio from being anti-apoptotic to pro-apoptotic, all indicative of initiation and progression of apoptosis involving mitochondrial dysfunction [1]. TBMS1-induced molecular events were related to mitochondria-induced intrinsic apoptosis and P21-cyclin B1/cdc2 complex-related G2/M cell cycle arrest [2]. TBMS1 combined with CDDP promoted cell apoptosis, decreased proliferation activity and increased cytosolic Ca2+ levels. Bcl-2 protein expression was down-regulated but Bax was up-regulated. Moreover, GST-π mRNA and protein expression were decreased. TBMS1 reduced the resistance of the cells to CDDP-induced cytotoxicity [4]. Treatment with TBMS1 resulted in dose- and time-dependent inhibition of proliferation, led to arrest in phase G2/M of the cell cycle and increased the levels of intracellular Ca2?. Furthermore, TBMS1 up-regulated the levels of the glucose-regulated protein 78/immunoglobuin heavy chain binding protein (GRP78/Bip), C/EBP homologous protein (CHOP), Bax, and cleaved caspase-3 and down-regulated the levels of Bcl-2 [5].in vivo: TBMS1 significantly inhibited the production of the pro-inflammatory cytokines, TNF-α, IL-6 and IL-1β in vitro and in vivo. Pretreatment with TBMS1 markedly attenuated the development of pulmonary edema, histological severities and inflammatory cells infiltration in mice with ALI [3].
17α-Neriifolin is a compound isolated from a methylene chloride extract of the seeds of Cerbera odollam[1].
Colistin A is a major component of Colistin. Colistin is a polymyxin antibiotic and can be used to combat infections caused by problematic gram-negative bacteria[1].
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity[1].
SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a Ki of 0.26 nM[1].
Fmoc-Ser-OH is a serine derivative[1].
Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza glabra, which inhibits aldose reductase with an IC50 of 320 nM.
N-(4-Nitrobenzoyl)glycine is a Glycine (HY-Y0966) derivative[1].
Tau Peptide (337-368) (Repeat 4 Domain) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.
Ladostigil (TV-3326) hemitartrate is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with an IC50 of 37.1 and 31.8 μM for MAO-B and AChE, reapectively. Ladostigil hemitartrate could increase cholinergic transmission, prevent the formation of ROS or their actions and be used for the research of depression and Alzheimer's disease[1][2].
Tafluprost(AFP-168) is an anti-glaucoma prostaglandin (PG) analog.Target:OthersTafluprost showed significant IOP-lowering effects without any safety concerns in patients with various types of glaucoma and OH in daily clinical practice and tafluprost is highly effective in any therapeutic patterns [1]. Tafluprost with reduced BAK has potential as a superior antiglaucoma drug, not only for its IOP-lowering effect, but also for its good corneal safety profile [2]. Tafluprost single-use vials treatment was effective in reducing IOP over the 3 years of this study, but visual field performance worsened by 10.3%-13.8% in patients with normal-tension glaucoma. Safety was satisfactory [3].
Pseudomonic acid D is a microbial inhibitor. Pseudomonic acid D potently inhibits mycoplasmas and bacterial pathogens. Pseudomonic acid D can be produced by fermentation with Pseudomonas fluorescens[1].
Conantokin R (Con-R) is an NMDA receptor peptide antagonist with an IC50 of 93 nM. Conantokin R binds Zn2+ and Mg2+ with Kds of 0.15 μM and 6.5 μM, respectively. Conantokin R shows anticonvulsant activity[1][2].
ICMT-IN-52 (compound 44) is an inhibitor of ICMT (IC50=0.052 μM)[1].
B-Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
N-Pivaloyl-L-tyrosine is an N-pivaloyl amino acid ester.
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes[1].
Rovadicitinib hydrochloride is a JAK inhibitor with an IC50 value <20 nM. Rovadicitinib hydrochloride also exhibits anti-inflammatory activity[1][2].
Anti-melanoma agent 1 (Compound 5m) is an anti-melanoma agent and induces cell apoptosis[1].