Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM[1]. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM[1][2].
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research[1].
ML382 is a potent, selective, positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1) with EC50 of 190 nM in cell based Ca2+ imaging assay; displays >100-fold selectivity versus MrgX2; enhances the ability of BAM8-22 to inhibit high-voltage-activated Ca2+ channels and attenuates spinal nociceptive transmission; effectively attenuated evoked, persistent, and spontaneous pain without causing obvious side effects; attenuates both evoked pain hypersensitivity and spontaneous pain in MrgprX1 mice; an invaluable research tool to study the role of MrgprX1 in chronic pain.
FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity[1].
16α-Hydroxydehydrotrametenolic acid is a triterpene Acid in fermented mycelia of edible fungus Poria cocos[1].
VGX-1027(GIT27) is an isoxazole compound that exhibits various immunomodulatory properties; reduce the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages.IC50 value: Target: immunomodulatorAdministration of VGX-1027 to NOD mice with spontaneous or accelerated forms of diabetes induced either by injection of cyclophosphamide or by transfer of spleen cells from acutely diabetic syngeneic donors markedly reduced the cumulative incidence of diabetes and insulitis. In addition, VGX-1027 given either i.p. or p.o. to CBA/H mice made diabetic with multiple low doses of streptozotocin successfully counteracted the development of destructive insulitis and hyperglycemia [1]. VGX-1027 appeared to spare T cell function as it was unable to modify the proliferation and/or secretion of IL-2, IFN-gamma and IL-4 induced in purified murine CD4+ T cells from stimulation with either CD3+CD28 or ConA [2]. VGX-1027 inhibited both proliferation of enterobacterial antigen-reactive CD4+CD25- T cells in vitro and the development of clinical and histological signs of colitis in vivo [3].
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM)[1][2].
bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs[1].
Deoxythymidine-5'-triphosphate (dTTP), a deoxynucleotide, can be used in deoxyribonucleic acid synthesis[1].
Tau Peptide (244-274) (Repeat 1 Domain) is aTau fragment.
Prednisolone disodium phosphate is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorPrednisolone irreversibly binds with glucocorticoid receptors (GR) alpha and beta for which they have a high affinity. Prednisolone can activate and influence biochemical behaviour of most cells. The steroid/receptor complexes dimerise and interact with cellular DNA in the nucleus, binding to steroid-response elements and modifying gene transcription. They induce synthesis of some proteins, and inhibit synthesis of others. Prednisolone exerted a delayed biphasic effect on the resistant CCRF-CEM leukemic cell line, necrotic at low doses and apoptotic at higher doses. At low doses, prednisolone exerted a pre-dominant mitogenic effect despite its induction on total cell death, while at higher doses, prednisolone's mitogenic and cell death effects were counterbalanced [1, 2].
Methyl cyclohexanecarboxylate is an endogenous metabolite.
4-(Benzyloxy)-2-nitrophenol is a synthetic building block that can be used in the synthesis of fluorescent ion indicators[1].
Dicloxacillin NaOH is a narrow-spectrum β-Lactam antibiotic of the penicillin class, is used to treat infections caused by susceptible Gram-positive bacteria, active against beta-lactamase-producing organisms such as Staphylococcus aureus.
Tyrphostin AG30 (AG30) is a potent protein tyrosine kinases (PTK) inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts[1][2].
H-D-Ser-OEt.HCl is a serine derivative[1].
ICMT-IN-9 (compound 47) is an inhibitor of ICMT (IC50=0.16 μM)[1].
D-Glucose-13C-5 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
7β-Hydroxycholesterol is an oxysterol that derived by the oxidation of cholesterol. 7β-hydroxycholesterol is a powerful inducer of oxidative stress, inducing dysfunction of organelles (mitochondria, lysosomes and peroxisomes) that can cause cell death[1].
α-Synuclein inhibitor 3 (Compound 7g) is a α-synuclein (α -Syn) aggregation inhibitor. α-Synuclein inhibitor 3 can be used for Parkinson’s disease research[1].
Blood group A pentasaccharide (A-Pentasaccharide), an oligosaccharide in urine, can inhibit the binding of anti-A antibody to blood group A substance[1].
Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities[1].
Guanidinoethyl sulfonate (Taurocyamine), a transport antagonist of taurine, induces much urinary taurine excretion with a resulting decrease in the tissue taurine content and readily produces taurine-deficient fetal rats in pregnant rats[1]. Guanidinoethyl sulfonate, a structural analogue of taurine, acts as a competitive inhibitor of taurine transport[2].
Gambogenic acid is an active ingredient in gamboge, with anticancer activity. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination[1].
MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells[1].
4-Tolueneboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Yakuchinone A is a natural product isolated from the fruit of Alpinia oxyphylla, which can induce apoptosis and has anticancer and anti-inflammatory activities[1].
(S)-2-Aminobutyramide-d3 (hydrochloride) is the deuterium labeled (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-5-(tert-butoxy)-5-oxopentanoic acid[1].
Cyanine5.5 maleimide (Cy5.5 maleimide) chloride is a potent fluorescent dye. Cyanine5.5 maleimide can be used as a protein stain[1].