Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].
Enuvaptan is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases[1].
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity[1].
Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM[1].
Pronase E is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
C6 NBD Lactosylceramide is a derivative of lactosylceramides, and can be used in lactosylceramide synthase assay as a fluorescent acceptor substrate. C6 NBD Lactosylceramide can also be used in cancer research[1][2].
OptoBI-1 is a photochromic TRPC3 agonist, which asts as a photopharmacological tool to control of neuronal firing[1].
E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent ROR isoforms selectivity (>5000-fold selectivity against human RORα and RORβ)[1].
Novel inhibitor of ER-to-cytosol protein dislocation, exhibiting anti-dengue and anti-Zika virus activity
E3 ligase Ligand-Linker Conjugates 7 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
L-Homopropargylglycine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-homopropargylglycine hydrochloride is an amino acid analog of methionine containing an alkyne moiety that can undergo a classic click chemical reaction with azide containing Alexa Fluor[1][2].
Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
A small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo; also reversibly attenuates fine touch perception in normal mice, reverses pathological mechanical hypersensitivity.
Fmoc-D-Pro-OH is a proline derivative[1].
Cdk5 Substrate is a biological active peptide. (substrate for the cdc2 protein kinase)
Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases[1].
Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP[1][2].
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum[1]. Halofantrine blocks HERG potassium channels[2].
LYPLAL1-IN-1 (Compound 11) is an selective covalent small-molecule inhibitors of Lysophospholipase-like 1 (LYPLAL1) with an IC50 of 0.006 μM. LYPLAL1-IN-1 increases glucose production[1].
Rhodamine 6G hydrazide (R6GH) is a fluorescent dye. Rhodamine 6G hydrazide can be used in selective colorimetric and fluorescent sensing[1].
Glyoxalase I inhibitor 2 (compound 26) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.5 µM. Glyoxalase I inhibitor 2 has the potential for the research of depression and anxiety[1].
HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants[1].
MurA-IN-2 (compound 37), a chloroacetamide fragment containing a primary aliphatic amine, is a potent MurA inhibitor with an IC50 value of 39 μM. MurA-IN-2 has antibacterial activity and inhibits the bacterial cell wall synthesis[1].
Angelicain (Norcimifugin) is a constituent of Cimicifuga foetida with anti-inflammatory activity[1].
P-T-P-S-NH2 is a short-chain peptide with an N-terminal proline[1].
N-Octylmaleimide is an alkylmaleimide, which can inhibit rat liver glucose 6-phosphatase[1].
Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia[1].