Alpha-ketoisocaproic acid-13C5 (sodium) is the 13C labeled Alpha-ketoisocaproic acid sodium[1].
Galanin-B2 (NAX-5055) has activity in the epilepsy model. Galanin-B2 can penetrate the blood-brain-barrier[1].
FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 nM and 0.5 nM for Plasmodium falciparum and human, respectively[1].
Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
mTOR Inhibitor 1 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR Inhibitor 1 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates[1].
TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).IC50 value: 50 nM [1]Target: Pim-1TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors.
Chitin synthase inhibitor 14 (compound 4n) is chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 14 has antifungal activity while possessed the potency against drug-resistant fungal variants[1].
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM[1].
2-Aminooxyethyliminodiacetic Acid Hydrochloride is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion[1].
Crenatine is an antibacterial agent. Crenatine is more effective against Gram-positive than Gram-negative bacteria[1].
PDE10-IN-2 is a PDE10 inhibitor with an IC50≦0.01 μM[1].
Mono-2-O-(p-toluenesulfonyl)-β-cyclodextrin is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Epoxomicin is a cell-permeable and irreversible proteasome inhibitor, primarily the chymotrypsin-like activity.
Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways[1].
Doxifluridine(Ro 21-9738; 5'-DFUR) is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM. IC50 value: 0.62 μM(PC9-DPE2 cell).Target: Nucleoside antimetabolite/analogDoxifluridine is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand.in vitro: 5'-DFUR's metabolic product(N3-Me-5'-dFUR) was found to be non-toxic in all the cell growth experiments performed. The absence of cytotoxicity could be explained by the observation that the metabolite was not recognized as a substrate by thymidine phosphorilase, the enzyme responsible for 5-fluorouracil (5-FU) release from doxifluridine, as ascertained by high-performance liquid chromatography/ultraviolet (HPLC-UV) analysis of the incubation mixture[1].in vivo: Administration of 200 mg of Furtulon to 23 beagle dogs, the plasma concentrations of doxifluridine, 5-FU, and 5-FUrd were measured simultaneously, using LC-MS/MS. The parent-metabolite compartment model with first-order absorption and Michaelis-Menten kinetics described the pharmacokinetics of doxifluridine, 5-FU, and 5-FUrd. Michaelis-Menten kinetics sufficiently explained the generation and elimination processes of 5-FU and 5-FUrd[2].Clinical trial: A phase II study of doxifluridine and docetaxel combination chemotherapy for advanced or recurrent gastric cancer was reported in 2009[3].
Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment[1][2].
Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells[1]. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities[3], protects against the development of arthritis in Rheumatoid arthritis (RA) animal models[2].
Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.Target: Calcium ChannelIsradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack[1]. Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. It is structurally related to felodipine, nifedipine, and nimodipine and is the most potent calcium-channel blocking agent of the DHP class. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells. It exhibits greater selectivity towards arterial smooth muscle cells owing to alternative splicing of the alpha-1 subunit of the channel and increased prevalence of inactive channels in smooth muscle cells. Isradipine may be used to treat mild to moderate essential hypertension [2].
Ac-DEVD-CHO is a specific Caspase-3 inhibitor with a Ki value of 230 pM.
Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
3-Phosphoglyceric acid barium is a metabolic intermediate in both glycolysis and the Calvin cycle. 3-Phosphoglyceric acid barium is involved in alveolar macrophage epigenetic regulation[1].
1,3,5-Triisopropylbenzene acts as a fuel and fuel additive. 1,3,5-Triisopropylbenzene is also used in lubricants and lubricant additives. 1,3,5-Triisopropylbenzene is used as a micelle expander[1].
ACAT-IN-6 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 200. ACAT-IN-6 potently inhibits NF-κB mediated transcription[1].
D-Galactose-4-O-sulfate sodium salt is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
A1AT modulator 2 (compound 33) is a modulator of A1AT (α-1 antitrypsin) with an IC50 value of ＞1.0 μM and an EC50 value of ＜0.4 μM. A1AT modulator 2 can be used for the research of infection and inflammation[1].
Adenosylhomocysteinase (SAHH; AHCY) is a highly conserved enzyme. Adenosylhomocysteinase reversible catalyzes S-adenosylhomocysteine (SAH) to adenosine and L-homocysteine. The serum exosomal Adenosylhomocysteinase level can be used as a prognostic biomarker in HBV-LC patients[1][2].
4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2)[1].
Fenuron-d5 is the deuterium labeled Fenuron. Fenuron is a phenyl urea-based widely used herbicide[1].