Norbraylin, a natural prenylated coumarin, is a PDE4D2 inhibitor with an IC50 value of 7.15 μM[1].
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD)[1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM[2].
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders[1].
IDE1 is an inducer of definitive endoderm 1 (IDE1).
NRC-16 is a biological active peptide. (pleurocidin-like cationic AMP)
Talc, a naturally occurring mineral composed primarily of magnesium, silicon and oxygen, is used in many cosmetics, from baby powder to blush[1][2].
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research[1][2][3].
Gonadorelin acetate is a man-made protein that is like a hormone in the body called gonadotropin-releasing hormone (GnRH). Target: GNRH ReceptorGonadorelin acetate is a synthetic decapeptide prepared using solid phase peptide synthesis. GnRH is responsible for the release of follicle stimulating hormone and leutinizing hormone from the anterior pitutitary.
N-(((9H-Fluoren-9-yl)methoxy)carbonyl)-N-(2-hydroxy-4-methoxybenzyl)glycine is a Glycine (HY-Y0966) derivative[1].
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM[1]. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC)[2].
Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM[1].
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism[1].
6-Methoxydihydrosanguinarine is an lkaloid isolated from the fruits of M.cordata. 6-Methoxydihydrosanguinarine shows strong cytotoxicity against MCF-7 and SF-268 cell lines with IC50 values of 0.61 μM and 0.54 μM, respectively[1].
G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer[1].
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC)[1].
2-C-methylene-myo-inositol oxide (NSC 45109), an inositol derivative, induces pseudohyphae formation in Saccharomyces spp[1].
Dihydrolanosterol-d7 is deuterium labeled Dihydrolanosterol. Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor[1].
DSPE-PEG Carboxylic acid sodium (MW 2000) is a PEG-lipid that can be used to form micelles as nanoparticles for drug delivery. DSPE-PEG Carboxylic acid sodium (MW 2000) increases the blood circulation time of liposomes[1].
SNT-207858 is a selective and orally available melanocortin MC-4 receptor antagonist with a 170-fold selectivity vs. MC-3 and a 40-fold selectivity versus MC-5. SNT-207858 has an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.
AKT-IN-13 (compound 4b) is a potent Akt inhibitor with IC50s of 1.6 nM, 2.4 nM and 0.3 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-13 can be used for researching anticancer[1].
Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes. Lobaplatin (D-19466) shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent[1][2].
DOTA-biotin is a DOTA-based small molecule hapten. DOTA-biotin has low tissue and whole-body retention in mice 4 h postinjection[1].
2’-Deoxy-2’-fluoro-b-D-arabinocytidine 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].
Chloramphenicol succinate is a proagent of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate also is an antibiotic. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity[1][2][3][4].
Cy7.5 is a fluorescence imaging (FI) agent (Ex=700-770 nm，Em=790 nm) as well as a magnetic resonance imaging (MRI) imaging agent. Cyanine dyes are used to label proteins, antibodies, peptides, and oligonucleotide[1].
Heptadecan-9-yl 8-((2-hydroxyethyl)amino)octanoate is a lipid that can be used for compound synthesis[1].
CP-060 is a potent Ca2+ antagonist, inhibits Ca2+ overload and possesses antioxidant and cardioprotective activities.
ASC-69 (APY69)is a potent and promising?PD-1/PD-L1 small-molecule inhibitor[1].