BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.
CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.IC50 value:Target: AMPAR agonistin vitro: Treatments with the ampakine CX614 markedly and reversibly increased brain-derived neurotrophic factor (BDNF) mRNA and protein levels in cultured rat entorhinal/hippocampal slices [1]. in contrast to cyclothiazide or IDRA 21, the Ampakine CX546 binds specifically to the agonist bound nondesensitized receptor, most likely acting by destabilizing the desensitized receptor conformation [2]. In binding tests, CX546 caused an approximately 2-fold increase in the affinity for radiolabeled agonists, whereas CX516 was ineffective [3]. in vivo: Intraperitoneal injections of CX546 increased hippocampal BDNF mRNA levels in aged rats and middle-aged mice [1]. Administration of the positive modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid receptors (AMPAR), CX546, during the conditioning phase only, improved the disrupted LI in mGluR5 knockout mice and facilitated LI in control C57BL/6J mice, given extended number of conditioning trails (four conditioning stimulus-unconditioned stimulus) [4].
Perindopril erbumine is a potent ACE inhibitor of which is used to treat high blood pressure, heart failure or stable coronary artery disease.Target: ACEPerindopril is a long-acting ACE inhibitor. It is used to treat high blood pressure, heart failure or stable coronary artery disease in form of perindopril arginine (trade names include Coversyl, Coversum) or perindopril erbumine (trade name Aceon). According to the Australian government's Pharmaceutical Benefits Scheme website, based on data provided to the Australian Department of Health and Aging by the manufacturer, perindopril arginine and perindopril erbumine are therapeutically equivalent and may be interchanged without differences in clinical effect. However the dose prescribed to achieve the same effect will differ due to different molecular weights for the two forms. Perindopril is one of the most prescribed inhibitors of angiotensin converting enzyme, has a large evidence base, which allows to use it in patients with hypertension, diabetes mellitus type 2, coronary heart disease and chronic heart failure. In this review, the author focused on the evidence of organoprotecting properties of perindopril that lie outside lowering blood pressure.
FLT3-IN-1 Succinate is a potent FLT3 inhibitor extracted from patent WO2015056683A1, compound example A.
(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol is a cucurbitane-type triterpenoid. (19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol has been tested to no effect against 5 cancer cell lines, MCF-7, HepG2, Du145, Colon205 and HL-60 by MTT assay[1].
Isobutylshikonin is a kind of shikonin pigments from hairy root culture of Lithospermum canescens[1].
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[1].
(2S)-2-[(tert-Butoxycarbonyl)amino]-3-(3-fluorophenyl)propionic acid is a phenylalanine derivative[1].
Acetyl-Tau Peptide (244-274) (Repeat 1 Domain) is a biologically active peptide.
Murrangatin is a coumarin that can be found in Murraya exotica[1].
Piperlactam S is an active compound. Piperlactam S can be isolated from Piper kadsura. Piperlactam S can be used for the research of chronic inflammation[1].
Lalistat 2 is a specific inhibitor of lysosomal acid lipase (LAL) with no effect on other forms of lipase[1].
Pimobendan hydrochloride is a selective inhibitor of PDE3 with IC50 of 0.32 μM.Target: PDE3Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). In human atrial cells, 100 μM pimobendan significantly increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50) of 1.13 μM. In rabbit atrial cells, Pimobendan increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells Pimobendan shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (1 mg/kg) also significantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with the control group, which shows no effect on myocardial necrosis, heart weight and body weight. Pimobendan suppresses expression of the intracardiac iNOS gene , causing reduction of intracardiac NO production.
9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 µM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo[1].
MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].
2-Aminopent-4-enoic acid is a Glycine (HY-Y0966) derivative[1].
AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
Glucocorticoids receptor agonist 1 is a potent anti-inflammatory, arylpyrazole-based glucocorticoid receptor agonist that does not impair insulin secretion.
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats[1][2].
N-Acetylprocainamide (Acecainide) hydrochloride is a class III antiarrhythmic, which blocks K+ channels[1].
9-(2’-O-Acetyl-5’-O-benzoyl-3’-O-methyl-beta-D-ribofuranosyl)-2,6-dichloropurine 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].
Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection[1]. DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
Azide-PEG3-Sulfone-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Neolinine is a diterpenoid alkaloid that can be isolated from the aerial parts of Aconitum carmichaeli[1].
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent[1][2].
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects[1][2].
Sarafotoxin S6a, a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC50 value of 7.5 nM[1].
UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders[1].
Dihydroguaiaretic acid, is isolated from the fruits of Schisandra chinensis with an anti-cancer activty[1].
GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra[1][2].