FICZ is a high affinity aryl hydrocarbon receptor (AhR) agonist with Kd of 70 pM.

Giredestrant, also known as GDC-9545 and RG6171, is a SERD. GDC-9545 is an orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD GDC-9545 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation.

TAK041(TAK 041) is a potent and selective GPR139 agonist with an EC50 of 22 nM. TAK-041 has the potential for the research of negative symptoms associated with schizophrenia.

Batefenterol Succinate is a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and β2-adrenoceptor agonist properties.

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