2-Aminoethan-1-ol-d4 hydrochloride is the deuterium labeled 2-Aminoethan-1-ol hydrochloride[1].
Rolusafine is an antifungal agent[1].
3-Epidehydropachymic acid, a lanostane triterpenoid, shows totoxicity effect against human acute monocytic leukemia cell line THP-1 (IC50=52.51 μM)[1].
DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner[1][2].
LHVS is a potent, non-selective cysteine protease inhibitor[1]. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion[2].
Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines.
Thymectacin (NB1011) is an agent selectively targeting tumor cells that have a high expression of thymidylate synthase (TS). Thymectacin is an aryloxy phosphoramidate derivative of BVdU (brivudin)[1][2].
1,5,15-Trimethylmorindol is an anthraquinone isolated from the leaves of Morinda citrifolia. 1,5,15- trimethylmorindol (25 μg/mL) does not show significant cytotoxic activity on the human T-cell leukemia cell line, Jurkat, by itself but it shows cytotoxicity (IC50 14.5-15.0 μg/mL) when combined with 0.5-1.5 μg/mL of TRAIL in the cell proliferation assay[1].
MES (2-Morpholinoethanesulphonic acid) potassium is a buffering agent in biology and biochemistry. MES potassium is one of the Good's buffers, the buffer capacity ranging pH 5.5-7.0. MES potassium is broadly used to regulate pH value for plants culture medium, reagent solution, and physiological experiments[1][2].
T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.
Phaseollidin is an antifungal agent that can be isolated from Phaseolus vulgaris L.[1].
Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer[1].
5-Ethoxymethyluridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Dammarenediol II (Compound 3) is a compound isolated from the resin of Boswellia freerana[1].
5(6)-Carboxynaphthofluorescein is a pH-dependent fluorophore. 5(6)-Carboxynaphthofluorescein shows good sensitivity in an alkaline pH range and it can be exploited in the construction of fiber-optic pH sensors. 5(6)-Carboxynaphthofluorescein can be used as a fluorescent pH indicator (Ex/Em=593/668 nm)[1].
PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay[1].
Lugrandoside is a nature product. Lugrandoside can be isolated from Digitalis davisiana Heywood[1].
Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect[1][2].
Clindamycin phosphate (Clindamycin 2-phosphate) hydrochloride is a broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin phosphate hydrochloride is the prodrug of Clindamycin (HY-B1455) with no antimicrobial activity in vitro but can be rapidly converted in vivo to the active parent drug, Clindamycin, by phosphatase ester hydrolysis. Clindamycin phosphate hydrochloride can be used for researching acne and bacterial vaginosis[1][2][3].
SB269970 is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.IC50 Value: 8.3 (pKi for 5-HT7) [1]Target: 5-HT7 receptorin vitro: 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. 5-HT(7) receptor mRNA was highly expressed in human hypothalamus, amygdala, thalamus, hippocampus and testis [1]. Cortical slices were loaded with [(3)H]-5-HT and release was evoked by electrical stimulation. 5-CT inhibited the evoked release of [(3)H]-5-HT in a concentration-dependent manner. SB-269970 had no significant effect on [(3)H]-5-HT release while the 5-HT(1B) receptor antagonist, SB-224289 significantly potentiated [(3)H]-5-HT release. In addition, SB-269970 was unable to attenuate the 5-CT-induced inhibition of release while SB-224289 produced a rightward shift of the 5-CT response, generating estimated pK(B) values of 7.8 and 7.6 at the guinea-pig and rat terminal 5-HT autoreceptors respectively [2].in vivo: Acute administration of SB-269970 (1 mg/kg) or amisulpride (3 mg/kg) ameliorated ketamine-induced cognitive inflexibility and novel object recognition deficit in rats. Both compounds were also effective in attenuating ketamine-evoked disruption of social interactions [3]. Pretreatment with a dose of SB-269970 (0.5 mM) that significantly affects sleep variables antagonized the LP-44 (2.5 mM)-induced suppression of REMS and of the number of REM periods [4].Toxicity: N/AClinical trial: N/A
Droxidopa(L-DOPS, SM5688) is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); capable of crossing the protective blood–brain barrierIC50 value: Target: The acute administration of droxidopa in PVL and BDL rats caused a significant and maintained increase in arterial pressure and mesenteric arterial resistance, with a significant decrease of mesenteric arterial and portal blood flow, without changing portal pressure and renal blood flow [1]. L-threo-dihydroxyphenyslerine (Droxidopa) is a pro-drug which has a structure similar to noradrenaline, but with a carboxyl group. It has no pressor effects in this form. It can be administered orally, unlike noradrenaline, and after absorption is converted by the enzyme dopa decarboxylase into noradrenaline thus increasing levels of the neurotransmitter which is identical to endogenous noradrenaline [2].
δ-Sleep Inducing Peptide is a neuropeptide, with antioxidant and anxiolytic properties.
Neoandrographolide is a diterpenoid from the Andrographis paniculata (Acanthaceae).
RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphan receptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer[1].
Helioxanthin (ACH126447) and its analogues exhibit significant in vitro antiviral activity against hepatitis B virus (HBV, EC50=1 uM) and flavivirus.IC50 value: 1/3/2 uM (EC50, HBV/HCV/HSV-1) [1]Target: Anti-HBV; Anti flavivirusin vitro: Helioxanthin and its analogues decreased cellular RNA levels of HBV and antigen expression as well as selective inhibition of HBV replication in a cell culture model [2]. Helioxanthin analogue 8-1 exhibited anti-DHBV activity as demonstrated by quantification of viral DNA, RNA, covalently closed circular DNA and protein synthesis. Analogue 8-1 did not affect the stability of cellular macromolecules and did not have a sustained antiviral effect after drug removal. When DHBV replication was induced, virus-harbouring cells were more susceptible to the cytotoxicity of 8-1 than non-induced cells [3].
4-Methylesculetin is an orally active natural coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity and reduces IL-6 level[1].
NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.In vitro: NAMI-A can significantly affect tumor cells with metastatic ability.The half lifetime of NAMI-A elimination from the lungs is longer than for liver, kidney, and primary tumor. NAMI-A bound to collagen is active on tumor cells as shown in vitro by an invasion test, using a modified Boyden chamber and Matrigel, and it inhibits the matrix metallo-proteinases MMP-2 and MMP-9 at micromolar concentrations. [1] The ruthenium drug NAMI-A inhibits the adhesion and migration of colorectal cancer cells. NAMI-A decreases α5β1 integrin expression and FAK auto-phosphorylation on Tyr 397. [2]In vivo: The reference for NAMI-A is 35 mg/kg/day. [1]
Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and an IL-2 variant that only binds IL-2Rβγ. Isotype: human IgG1[1].
Trimethoprim sulfate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim sulfate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim sulfate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim sulfate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc[1][2][3][4].