Rifampicin-d3 (Rifampin-d3) is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities[1][2].
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects[1][2].
HDAC-IN-52 is a pyridine-containing HDAC inhibitor, with IC50s of 0.189, 0.227, 0.440 and 0.446 μM for HDAC1, HDAC2, HDAC3, and HDAC10, respectively. HDAC-IN-52 can be used for the research of cancer[1].
AMCA-X SE is a fluorescent molecules compounded for the tagging of biomolecules with a maximum absorption of 354 nm and a maximum emission of 442 nm[1].
Merodantoin has significant antitumor activity in vitro and in vivo, and has less toxicity to normal cells and tissues[1].
D-Fructose-13C (D(-)-Fructose-13C) is the 13C labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants.
Boc-Ile-ONp is an isoleucine derivative[1].
Aurantiamide is an orally active constituent of Portulaca oleracea L and has various biological activities, including antioxidant, antiplatelet, anti-inflammatory, and antitumor activities[1].
Caryatin is a natural product found in Rhododendron simiarum, and Aeonium decorum. Caryatin shows anti-tumor activity[1].
5'-O-DMT-N4-Ac-dC (N4-Acetyl-2'-deoxy-5'-O-DMT-cytidine, compound 7), a deoxynucleoside, can be used to synthesize of dodecyl phosphoramidite which is the raw material for dod‐DNA (amphiphilic DNA containing an internal hydrophobic region consisting of dodecyl phosphotriester linkages) synthesis[1][2].
GSK-199 hydrochloride is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay; shows high specificity for PAD4 over PAD1/2/3/6; affects cellular citrullination and mimic the deficiency in NET production in mice; significantly decreases in complement C3 deposition in both synovium and cartilage in mice.
Pentamidine Dihydrochloride(MP601205 dihydrochloride) is an antimicrobial agent.Target: AntiparasiticPentamidine Dihydrochloride has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1[1][2].
Ferulic acid (4-hydroxy-3-methoxycinnamic acid) is a phenolic compound present in several plants with claimed beneficial effects in prevention and treatment of disorders linked to oxidative stress and inflammation.IC50 value:Target: 5-HT ReceptorIn vitro: In the present study we have showed that pre-treatment with Ferulic Acid (FA) reduces NO accumulation in the culture medium of LPS-induced macrophage cells. Moreover, real-time experiments have revealed that FA has an inhibitory effect at the transcriptional level on the expression of some inflammatory mediators such as IL-6, TNF-α and iNOS and an activation effect on the expression of some antioxidant molecules such as Metallothioneins (MT-1, MT-2). Importantly, we have found that FA reduced the translocation of NF-E2-related factor 2 (Nrf2) and nuclear transcription factor-κB (NF-κB) into the nuclei through a reduction of the expression of phosphorylated IKK and consequently inhibited IL-6 and NF-κB promoter activity in a luciferase assay [1]. FA treatment significantly, although not completely, protected the cells against lead acetate-induced neurite outgrowth inhibition. The effects of FA could be blocked by PD98059, zinc protoporphyrin (Zn-PP), and Nrf2 shRNA. In addition, FA induced heme oxygenase 1 (HO-1) gene expression, enhanced antioxidant response element (ARE) promoter activity, promoted ERK1/2 phosphorylation, and Nrf2 translocation in PC12 cells exposed to lead acetate. ERK1/2 locate upstream of Nrf2 and regulate Nrf2-dependent HO-1 expression in antioxidative effects of FA [2].In vivo: We aimed to verify the possible antidepressant-like effect of acute oral administration of Ferulic acid produced an antidepressant-like effect in the FST and TST (0.01–10 mg/kg, p.o.), without ccompanying changes in ambulation. The pretreatment of mice with WAY100635 (0.1 mg/kg, s.c., a selective 5-HT1A receptor ntagonist) or ketanserin (5 mg/kg, i.p., a 5-HT2A receptor ntagonist) was able to reverse the anti-immobility effect of ferulicacid (0.01 mg/kg, p.o.) in the TST. The combination of fluoxetine (5 mg/kg, p.o.), paroxetine (0.1 mg/kg, p.o.) or sertraline (1 mg/kg, p.o.) with a sub-effective dose of ferulic acid (0.001 mg/kg, p.o.) produced a synergistic antidepressant-like effect in the TST, without causing hyperlocomotion in the open-field test. ferulic acid in the forced swimming test (FST) and tail suspension test (TST) in mice [3].
Benzonatate (Benzononatine) is a peripheral oral antitussive that dampens the activity of cough stretch receptors. Benzonatate has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite[1][2].
Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.
Iodoacetyl-LC-biotin is a biotinylated electrophile probe that can be used to investigate the scope and characteristics of protein covalent binding to subcellular proteomes[1][2].
8-Aza-7-deazguanosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Amifampridine (3,4-Diaminopyridine) phosphate is an orally active potassium channel blocker (PCB), can block presynaptic potassium channels[1]. Amifampridine phosphate can be used in Lambert-Eaton myasthenic syndrome (LEMS) research[1].
BB 0305179 (compound 59) is a potent anti-prion agent, with an IC50 of 4.7 μM. BB 0305179 inhibits the toxicity of a specific PrP mutant carrying a deletion in the hydrophobic domain [1].
Antibacterial compound 2 is a useful antibacterial agent extracted from patent US5652238, compound example 9.
Sporidesmolide V is a cyclodepsipeptide compound isolated from the cultures of Pithornyces chartarum[1].
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression[1].
N-Chloroacetyl-DL-alanine is an alanine derivative[1].
Ras modulator-1 is a modulator of Ras. Ras modulator-1 is an active compound extracted from patent US20120302581[1].
DB0662 is a compound for kinase-targeted protein degradation and can be used in studies of diseases mediated by abnormal kinase activity, as well as for the identification of degradable kinases and optimal kinases[1].
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively[1]. MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells[1].
ET-JQ1-OH is an allele-specific BET inhibitor[1].
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease[1].