3,4-Dichloroisocoumarin is a potent serine-protease inhibitor that inhibits chymotrypsin-like activity[1].
D-Phenylalanine is the synthetic dextro isomer of phenylalanine. D-Phenylalanine inhibits biofilm development of Pseudoalteromonas sp. SC2014[1].
Taxezopidine G is a natural product, that can be isolated from the seeds and stems of Japanese Yew Taxus cuspidata[1].
LpxH-IN-AZ1, a sulfonyl piperazine compound, is a potent UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH inhibitor. LpxH-IN-AZ1 is a potent inhibitor of Klebsiella pneumoniae LpxH with IC50 of 0.36 μM [1].
ML-SA5 is a potent TRPML1 cation channel agonist that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and is more potent than ML-SA1. ML-SA5 has anticancer activity and can tumour growth[1].
Cholesterol-d4 is deuterium labeled Cholesterol. Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins[1][2]. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist[3].
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist[1][2][3][4].
3β-Hydroxylanosta-8,24-dien-21-al is a lanostane-type triterpene. 3β-Hydroxylanosta-8,24-dien-21-al can inhibit the tumor promotion, reducing the percentage of mice bearing papillomas[1].
Vibecotamab (XmAb14045) is a potent bispecific antibody against CD123 and CD3 that stimulates T cell-mediated targeted killing of CD123-expressing cells. Vibecotamab has antitumor activity and can be used in acute myeloid leukaemia studies[1].
EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC50 of 0.34 μM. EGFR-IN-67 shows anticancer activity[1].
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
2,3-Dibromosuccinic acid is the inactive isomer of (±)-2,3-Dibromosuccinic acid (HY-133681), and can be used as an experimental control. (±)-2,3-Dibromosuccinic acid is the key intermediate in the synthesis of dicarboxylic acid derivatives[1].
DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research[1].
GDC-6599 (Example 8) is an orally active TRPA1 inhibitor. GDC-6599 can be used to study TRPA1-mediated diseases such as pain[1].
Sarcosine-d3 (N-Methylglycine-d3) is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
Flemiphilippinin A is a prenylated isoflavone isolated from Flemingia philippinensis[1].
Antibacterial agent 61 (example 27) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Vemurafenib is a novel and potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively.
N,N'-Dinitrosopiperazine-d8 is the deuterium labeled N,N'-Dinitrosopiperazine[1]. N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568[2].
Antitumor agent-F10 (Compound F10) is a camptothecin derivative. Antitumor agent-F10 is an orally–bioavailable and potent antitumor agent. Antitumor agent-F10 displays lower acute toxicity than SN-38 does and the solubility of F10 reached 9.86 μg/mL[1].
CAY10404 is a potent and highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM. CAY10404 exhibits no inhibition of COX-1 (IC50>500 µM)[1]. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[2][3].
Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity[1].
Clofentezine, a growth inhibitor, has sublethal effects on life-table parameters of Tetranychus urticae Koch females.
Rosmarinic acid racemate is the racemate of Rosmarinic acid. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.
Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system.
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca2+-activated K+ channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels[1][2][3].
BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
Fmoc-Glu(OtBu)-OH-15N is a 15N-labeled Fmoc-L-Val-OH[1].
Honokiol DCA (Honokiol dichloroacetate) is a dichloroacetate analog of Honokiol. Honokiol DCA can inhibit the growth of human prostate cancer cells in vitro and suppress the androgen receptor (AR) protein level[1].