Vazegepant (BHV-3500) hydrochloride is a highly soluble CGRP receptor antagonist. Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation.

DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM..

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) with IC50 values of 8nM and 8.2nM for I-IP-10 and I-ITAC, respectively. AMG 487 prevents the chemokines I-IP-10 and I-ITAC from binding to CXCR3. In the cellular assays, AMG 487 inhibits CXCR3-mediated cell migration with IC50 values of 8nM, 15nM and 36nM for I-IP-10, I-ITAC and MIG, respectively.

Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research.

JNJ-18038683 is a potent, selective 5-HT7 receptor antagonist with pKi of 8.19 and 8.20 for rat and human 5-HT7 in cell-based assays.

Aumitin is a novel potent autophagy inhibitor with IC50 of 124 and 244 nM against starvation- and rapamycin- induced autophagy respectively, targets mitochondrial complex I.

Azidoacetic acid NHS ester is a compound containing an azide group and an NHS ester. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. The NHS ester can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.

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).