PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.C391 blocks both PAR2 Ca2+ and MAPK signalling pathways activated by peptidomimetics and/or proteinase activation.C391 effectively attenuated compound 48/80-induced thermal hyperalgesia in vivo.C391 blocked A. alternata-induced, PAR2-dependent Ca2+ and MAPK signalling in 16HBE14o- cells, as well as β-arrestin recruitment in HEK 293 cells.C391 effectively attenuated A. alternata-induced inflammation, mucus production, mucus cell hyperplasia and airway hyperresponsiveness in acute allergen-challenged murine models.

DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM).

DDAO is a promising near-infrared (NIR) red fluorescent probe with tunable excitation wavelength (600-650 nm) and long emission wavelength (λem = 656 nm). DDAO can de desiged for detection of the activities of different enzymes such as β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin and esterases.

A novel Non-competitive AMPA/kainate antagonist.

Selective cell permeable phosphatidylinositol 3-kinase (PI3K) inhibitor

Benzamil hydrochloride is a specific and potent sodium channel (ENaC) blocker.

H2DCFDA is a fluorescent cell permeabl ROS indicator.

TTA-A2 is a potent, selective and orally active t-type voltage gated calcium?channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

Dizocilpine, a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.

BMS-986449 is a CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors.

Naspm(1-Naphthylacetyl spermine) is a potent and selective Ca2+ permeable AMPA receptor(Ca-perm AMPAR) blocker. IC50 value: Target: CP-AMPAR blocker Naspm is a selective blocker of Ca(2+)-permeable GluA2-lacking AMPA receptors, reduced MNNG-induced CA1

A potent pan HER/VEGFR inhibitor with IC50 of 5/20/60/50 nM for EGFR/HER2/ERBB4/VEGFR2 respectively.

Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH), shows greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion..

Fluoxymesterone is an Androgen. The mechanism of action of fluoxymesterone is as an Androgen Receptor Agonist.

Sitostanol is a saturated sterol found in a variety of plants, including corn, wheat, and rice and reduces cholesterol uptake in rats and rabbits.

SD133 (Sd-133) is a drug-like small molecule inhibitor of adhesion molecule cadherin 11 (CDH11), binds specifically to the CDH11 binding pocket with KD of 25.2 uM in SPR assays.

STAT3 inhibitor N4 is a small molecule capable of inhibiting the STAT3 SH2 domain with IC50 of 0.57 uM, SPR KD of 1.04 uM, inhibits STAT3 dimerization and transcription in vitro and suppresses pancreatic cancer in vivo.N4 suppresses STAT3 activation in pancreatic cancer cells, suppresses pancreatic cancer cell growth, migration, and induces apoptosis.N4 (20 mg/kg, i.p.) suppresses pancreatic cancer growth, exhibits potent anti-metastatic activity in a pancreatic cancer liver metastasis mouse model, and prolongs survival of tumor-bearing mice.

Leuprorelin (Leuprolide) is a GnRH analog and agonist of GnRH receptor, interrupts the normal pulsatile stimulation and desensitizing of the GnRH receptors..

An E3 ligase ligand-linker conjugate for PROTAC...

Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.

10-Nitrooleic acid (CXA-10), a nitro fatty acid, has potential effects in disease states in which oxidative stress, inflammation, fibrosis, and/or direct tissue toxicity play significant roles.

TGP-29b-066 (Targapremir-29b-066) is a specfic small-molecule miR-29b inhibitor that targets miR29b hairpin precursor (pre-miR-29b), selectivity and effectively decreases miR-29b expression levels in C2C12 myoblast, attenuates muscle atrophy in vitro and

Myoseverin is an inducer of the reversible fission of multinucleated myotubes into mononucleated fragments, affecting the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration.

Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors. Rotigotine exhibits antiparkinsonian acitivity.

PF-06835919, also known as MDK1846, is a potent ketohexokinase (KHK) inhibitor. PF-06835919 is reported in patent US 20170183328 A1, example 4. Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in humans. Since ketohexokinase (KHK) is the principal enzyme responsible for fructose metabolism, identification of a selective KHK inhibitor may help to further elucidate the effect of KHK inhibition on these metabolic disorders.

Vonafexor (EYP001) is a selective FXR agonist with anti-HBV effects.

Pax2 inhibitor EG1 (EG1) is a potent, small molecule inhibitor of Pax2 mediated transcription activation, effectively blocks Pax2 activity and DNA binding with Kd of 1.35-1.5 uM; inhibits Pax2 mediated expression with IC50 of 10 uM, and inhibits proliferation of Pax2 positive renal and ovarian cancer cell lines but has little effect on Pax2 negative cancer cells; inhibits embryonic kidney development.

GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).

MG-115(MG 115) is an inhibitor of NFκB in the cytoplasm by acting on IKK or the proteasome.