Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction[1][2].
Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors[1][2].
AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis[1].
Sperabillin A (dihydrochloride)is new inhibitors ofglutathione S-transferaseisolated from the culture broth ofStreptomyces sp[1].
LDL-IN-3 is an anti-atherosclerotic compound extracted from patent WO/2005/039596A1, example C25 and patent US 6133467, example 3.
lucPpy-IN-1 (compound 9) is an ATP-dependent luciferase from Photinus pyralis (lucPpy) inhibitor with an IC50 value of 4.0 µM. lucPpy-IN-1 can be used for the research of target’s druggability[1].
Eptifibatide acetate is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity[1].
5-FAM-Pro-Leu-OH is a biological active peptide. (Used as MMP fluorescent reference standard)
Odoriflavene is a phenolic compound found in the root heartwood of Dalbergia odorifera T. Chen (Leguminosae)[1].
BRD0705 (BRD-0705) is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM); displays excellent selectivity in a penal of 311 kinases, the CDK family of CDK2, CDK3 and CDK5) are most potently inhibited with IC50 of 6.87, 9.74 and 9.20 uM (87-, 123-, and 116-fold selectivity relative to GSK3α); inhibits GSK3α kinase function, impairs GSK3α Tyr279 phosphorylation in a time- and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation, and does not stabilize β-catenin, induces myeloid differentiation and impairs colony formation in AML cells, with no apparent effect on normal hematopoietic cells; impairs leukemia initiation and prolongs survival in AML mouse models.
Strictosidine, the central intermediate in monoterpene indole alkaloid (MIA) biosynthesis, undergoes a series of reactions to produce over 3,000 known MIAs such as Vincristine, Quinine (HY-D0143), and Strychnine[1].
EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation[1].
Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract[1][2].
N-(3-Phenylpropanoyl)pyrrole is a natural product, that can be isolated from the fresh roots, fruits and leaves of Piper sarmentosum[1].
Glycidamide is the genotoxic metabolite of Acrylamide. Glycidamide can react with proteins, such as hemoglobin, or with DNA, and induces genotoxic effects[1].
GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates[1][2].
LNP023 is a highly potent factor B (FB) inhibitor with an IC50 value of 10 nM. LNP023 shows direct, reversible, and high-affinity binding to human FB (KD=7.9 nM)[1].
2’-Deoxy-N2,N2-diethyl guanosine 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].
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.IC50 value: 0.19 nM (Ki) [1]Target: M3 muscarinic receptorin vitro: SVT-40776 is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 was the most potent in inhibiting carbachol-induced bladder contractions of the anti-cholinergic agents tested, without affecting atrial contractions over the same range of concentrations. SVT-40776 exhibited the highest urinary versus cardiac selectivity (199-fold) [1]. SVT-40776 has a much higher binding affinity (K(d) = 0.4 nM) to M5 mAChR than that of solifenacin (K(d) = 31 nM) with the same reeptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to SVT-40776 is in good agreement with the experimentally derived binding free energy change (-2.58 kcal/mol), suggesting that our modeled M5 mAChR structure and its complexes with the antagonists are reliable [2].in vivo: In the guinea pig in vivo model, SVT-40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v), without affecting arterial blood pressure [1].
IDO1-IN-17 (I-4) is an IDO1 inhibitor, with an IC50 of 0.44 μM in hela cells[1].
Pseudoginsenoside RT5 is isolated from Panax quinquefolium[1].
2-Furoic acid-d3 is the deuterium labeled 2-Furoic acid[1]. 2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation[2]. 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats[3].
Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
5'-O-DMT-ibu-rG is a useful model for a new class of DNA binding molecules for the development of potent and selective anti-cancer agents[1].
DBCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Miglitol-d4 (BAY1099-d4) hydrochloride is the deuterium labeled Miglitol. Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose[1][2].
Nα,Nε-Bis(2,4-dinitrophenyl)-L-lysine is a lysine derivative[1].
Effusanin E is a diterpenoid. Effusanin E, a 7α, 20-Epoxy-ent-kauranoid, can be obtained from Isodon parvifolius. Effusanin E can be used for the research of cancer[1].
Bis-sulfone-PEG3-Azide is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Calcium glycerophosphate is an inhibitor of intestinal alkaline phosphatase F3. Calcium glycerophosphate is a source of calcium and phosphorus in total parenteral nutrition solutions[1][2].