Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM.Target: HIV proteaseLopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.
LGK974 is a potent and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
3’-Deoxy-N6-methyladenosine 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].
(16R)-E-Isositsirikine is an indole alkaloid compound from Catharanthus roseus Tissue Cultures IV1[1].
Fmoc-Lys(5'-FAM)-OH is a lysine derivative[1].
Netarsudil mesylate is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.
3-Methylcatechol is a building block in the chemical synthesis produced by Pseudomonas putida MC2[1].
Trisulfo-Cy5-Alkyne is a click chemistry reagent containing an azide group. Trisulfo-Cy5-Alkyne can participate in copper-catalyzed Click Chemistry reactions. Trisulfo-Cy5-Alkyne is a near infrared (NIR) fluorescent dye[1].
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM[1]. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor[2].
Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase[1].
Pomalidomide 4'-alkylC5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.
NUC-7738 is a phosphoramidate transformation of cordycepin (3’-deoxyadenosine; 3’-dA), a derivative of adenosine that was first isolated from Cordyceps sinensis.
Benzyl-PEG4-Azido is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Quinolactacin A1 is a potent acetylcholinesterase (AChE) inhibitor from solid state fermentation of Penicillium citrinum 90648. Quinolactacin A1 can be used for the research of Alzheimer disease[1].
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[1].
CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM)[1].
Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively[1].
Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT[1].
LY285434 is a suitable angiotensin II receptor antagonist.
N-Benzyl-N-bis-PEG4 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Chemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis[1][2][3].
Imatinib is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
Coriatin can be isolated from L. parasiticus and has antischizophrenia activity[1].
TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities[1].
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
HL23 is a histone deacetylase (HDAC) inhibitor with activity against hepatocellular carcinoma (HCC). HL23 enhances acetylation of the TXNIP promoter and upregulates TXNIP expression, thereby mediating potassium channel activity and triggering TXNIP-dependent potassium deprivation. HL23 inhibits HCC progression and metastasis and has a synergistic effect with Sorafenib (HY-10201) and is more potent than Sorafenib+Vorinostat (HY-10221)[1].
TRH-AMC is a fluorogenic substrate used in a coupled assay for thyrotropin-releasing hormone(TRH)-degrading ectoenzyme[1].
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity[1][2][3][4][5].