SWN41522, also known as DUPA and FN11, is a potent Urea-​Based Inhibitor of Glutamate Carboxypeptidase II (NAALADase). In vivo antitumor tests using U-​87 glioblastoma xenograft showed that FN11 reduced tumor vol. to a value of ∼0.4-​0.6 (at 10 or 100 μM) after 4 days treatment, and ∼ 1.0 (at both dosages) after 7 days treatment. The antiangiogenesis activity of FN11 was examd. with similarly grown tumors, and revealed a preponderance of avascular and low vascular areas in tumors treated with FN11 at 100 μM. It was first reported in patent WO 2000064911 and Journal of Medicinal Chemistry (2001), 44(3), 298-301.

Difelikefalin is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor.

A polyamine oxidase (PAO) inhibitor that inhibits spermine oxidase and N1-acetylpolyamine oxidase with IC50 of 6.1 and 0.02 uM, respectively.

Novel Nox inhibitor，N2-(3,4-Dimethylphenyl)-6-((4-(p-tolyl)piperazin-1- yl)methyl)-1,3,5-triazine-2,4-diamine

Avanafil Impurity 8

CAY10526 is a selective inhibitor of mPGES-1. It also acts as an inhibitor of the NF-κB signaling pathway.

ML353 (VU0478006) is a ovel Silent Allosteric Modulator (SAM) of the Metabotropic Glutamate Receptor 5.

Z-ASTD-FMK is a cell-permeant and irreversible inhibitor of endothelial monocyte-activated polypeptide II (EMAP II).

Z-FF-FMK is a cell-permeant and irreversible inhibitor of cathepsin B and cathepsin L.

dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression. As an efficient degrader of this unique class of acetyltransferases, dCBP-1 is a useful tool alongside domain inhibitors for dissecting the mechanism by which these factors coordinate enhancer activity in normal and diseased cells.

2-Bromohexadecanoic acid (2-BP, 2-bromopalmitate) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins.

Dideoxyadenosine is konwn as 2′,3′-Dideoxyadenosine (ddA), a specific adenylyl cyclase inhibitor, is useful in biological process and pathway studies involving adenylyl cyclase activity and cAMP pool modulation.

MCULE-3408819416|DC Chemicals

Homo-VK-II-36 is a carvedilol analogue. It acts by inhibiting store-​overload-​induced calcium release (SOICR) through the RyR2 channel.

KYN-101 is a novel potent and selective inhibitor of aryl hydrocarbon receptor (AHR) (IC50 of 22 nM in the human HepG2 DRE-luciferase reporter assay and 23 nM in the murine Hepa1 Cyp-luc assay).

Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6).

Coumarin-TMP-Halo is a specific fluorescent protein labeling agent.

DL5H3 is a biochemical.

BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 81 nM. BAY-8400 shows synergistic activity of DNA-PK inhibition when combined with DNA damage inducing cancer therapy, like targeted alpha radiation.

Novel upregulator of TRIB1 expression, leading to reprogramming of hepatic lipoprotein metabolism from lipogenesis to scavenging

Novel potent SIRT6 activator against whole histone substrate

Novel potent and selective antagonist of human Complement C3a receptor

Novel autophagy inhibitor, selectively targeting cholesterol transfer protein GRAM domain-containing protein 1A (GRAMD1A), and directly competing with cholesterol binding to the GRAMD1A StART domain

The first-in-class dual inhibitor of ENL (Kd = 754 ± 45 nM) and its paralog AF9 (Kd = 523 ± 53 nM)

Novel potent inhibitor of the GRK2--​dependent bovine tubulin oxidation