Sulfoxone (Aldesulfone) disodium is an orally active sulphonamide antibiotic that is used against leprosy. Sulfoxone disodium can also be used in study of dermatitis herpetiformis[1][2].
RPE65-IN-1(Compound 16e) is a potent RPE65 inhibitor, which can be used in retinopathy-related research[1].
GSK329 is a potent and selective diarylurea inhibitor of the cardiac-specific kinase TNNI3K. GSK329 exhibits positive cardioprotective outcomes in the model of ischemia/reperfusion cardiac injury[1].
Isoprenaline hemisulfate is a non-selective β-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities[1][2][3][4][5].
Boromycin is a compound isolated from is a compound isolated from Streptomyces antibioticus[1].
4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM.
Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor[1][2].
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively)[1]. AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine[2].
4-Chlorothiobenzamide-d4 is the deuterium labeled 4-Chlorothiobenzamide[1].
[Mpr7, DAla9] ANP (7-28), amide, rat is an atrial peptide[1].
Gastrin-1, rat (Rat Gastrin-17) is a peptide hormone, and can stimulate gastric acid secretion potently[1].
Thalidomide-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Massoia lactone ((±)-Massoia lactone) is a coconut and creamy fragrant compound mianly isolated from Cryptocarya massoy. Massoia lactone is also a fragrant biosurfactant produced by a fungus Aureobasidium pullulans[1].
1,2-Diheptadecanoyl-sn-glycero-3-phosphorylcholine (DHPC) is a biologically active phospholipid compound and a derivative of phosphatidylcholine (PC)[1].
6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor. 6-O-Isobutyrylbritannilactone, a sesquiterpene, can be isolated from the flowers of Inula britannica. 6-O-Isobutyrylbritannilactone inhibits IBMX (HY-12318)-induced melanin production in B16F10 cells. 6-O-Isobutyrylbritannilactone also regulates ERK, PI3K/AKT, and CREB, shows antimelanogenic activity in zebrafish embryos models[1].
MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM, 10-fold increase in inhibitory activity over MI-463 and MI-503; markedly reduces cell growth of murine bone marrow cells transformed with MLL-AF9 with GI50 of 34 nM, demonstrates potent on target activity in MLL leukemia cells with GI50 values of 36 nM in MV4;11 (harboring MLL-AF4 fusion protein) and 61 nM in MOLM13 (harboring MLL-AF9); downregulates the MLL fusion protein target genes, HOXA9 and MEIS1, at 100 nMin MV4;11 human MLL leukemia cells; strongly inhibits leukemia progression in vivo.
Dotinurad is a potent uricosuric agent, with an IC50 of 3.6 µM for uric acid[1].
Heparin is a highly sulfated glycosaminoglycan,that is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule.
Doxifluridine-d2 is the deuterium labeled Doxifluridine[1]. Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
Setiptiline is a serotonin receptor antagonist.IC50 value:Target: 5-HT receptorSetiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine. From Wikipedia.
Ergosta-7,22-dien-3-on is a lanosterane isolated from the fruiting bodies of Ganoderma lucidum. ent-16-Kaurene-3b,15b,18-triol inhibits platelet aggregation[1][2].
Bliretrigine is a sodium channel blocker. Bliretrigine has the effect of relieving pain[1][2][3].
ZLN005 is a novel transcriptional regulator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).IC50 value:Target: PGC-1αin vitro: ZLN005 increases expression of the PGC-1α gene in L6 myotubes. ZLN005 increased PGC-1α mRNA levels in a dose-dependent manner; 20 μmol/L ZLN005 caused a threefold increase over the control after 24 h. At 10 μmol/L, the PGC-1α mRNA levels were increased to almost the same extent at 16 to 48 h [1]. ZLN005 did not increase the expression of the PGC-1α gene in rat primary hepatocytes. AMP-activated protein kinase is involved in the mechanism inducing PGC-1α in L6 myotubes [1]in vivo: An insulin tolerance test revealed that treatment with ZLN005 significantly decreased insulin resistance in db/db mice, as evidenced by the approximately 18% decrease in the AUC. A PTT also was performed in db/db mice, and ZLN005 improved pyruvate tolerance, as evidenced by the 16% decrease in the AUC. In db/db mice, plasma NEFA and triglyceride levels were decreased by 20% and 37%, respectively, and cholesterol was decreased by 10% with ZLN005 treatment. Plasma insulin and β-hydroxybutyrate content, liver/bodyweight index and adipose composition, and muscle and liver triglyceride levels, however, were not ameliorated by treatment with ZLN005 or metformin [1].
A novel potent, selective mGluR2 positive allosteric modulator with EC50 of 199 and 206 nM for human and rat mGlu2, respectively, without exerting agonist activity; has negligible activities for other mGlu receptors, including mGlu3 receptor; potentiates the mGlu2 receptor-mediated presynaptic inhibition of glutamate release, inhibits both MK-801- and ketamine-increased cortical γ band oscillation in the rat cortical electroencephalogram; significantly inhibits both ketamine- and methamphetamine-increased locomotor activities in mice.
NBD-PE is an effective lipid fluorescent probe (Excitation/Emission: 465/535 nm; Color: Green). NBD-PE offers a wide array of applications in membrane and cell biology[1][2][3].
Aminooxy-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
BAY 1161909 is a potent Mps1 inhibitor, with an IC50 of < 1 nM.
2-Amino-3-carboxy-1,4-naphthoquinone is the electron transfer mediator. 2-Amino-3-carboxy-1,4-naphthoquinone changes glucose metabolism of the homofermentative lactic acid bacteria[1].
Tenuiphenone B is a benzophenone isolated from the ethanolic extract of Polygala tenuifolia.
Methyl salvionolate A is a potent inhibitor of HIV-1. Methyl salvionolate A inhibits P24 antigen in HIV-1 infected MT-4 cell with an EC50 of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with IC50s of 50.58, 10.73 and 7.58 μg/ml, respectively[1].