Novel lysophosphatidic acid receptor 3 (LPA3) agonist

Orphan nuclear receptor DAF-12 ligand, inhibiting the dauer-promoting activity of DAF-12

Novel water-sensitive probe, demonstrating superior sensitivity for detecting modulation of water microsolvation, structural conformation during oligomer formation and 5FUrd binding to both wild type and mutant SOD1

Building Block

Negative control for RSL3

Potent antagonist of GluN2B-NMDA receptors (Ki = 5.8 nM), inhibiting ion flux in two-electrode voltage clamp experiments (IC50 = 223 nM)

Novel prodrug of the sigma (σ) ligand haloperidol metabolite II conjugated with the histone deacetylase (HDAC) inhibitor valproic acid, demonstrating antiangiogenic activity

Novel profluorescent RAMOSUS3 (RMS3) probe with strigolactone-like bioactivity

Potent and selective 5-HT2 serotonin receptor agonist

Inhibitor of ADP-induced platelet aggregation; anti-thrombotic

Novel potassium channel opener

Novel angiogenesis inhibitor, regulating endothelial cell fate and angiogenesis

Novel probe for mycobacterial and fungal carbonic anhydrase

Catecholamine-depleting agent, actively against the 3 major monoamines in the CNS

Novel potent anti-malarial agent against multiple resistant strains of P. falciparum in vitro and show no cytotoxicity to mammalian cells

Folate-PEG2-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Folate-PEG3-amine is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

A potent and selective Adenosine receptor A2A agonist

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.

JMV 2959 (AEZS-123) is a potent ghrelin receptor (GHS-R1A) antaognist with binding IC50 of 32 nM.

Nutlin-3a is arbitrarily referred to as enantiomer a because it appears as the first peak from chiral purification of racemic nutlin-3 and its absolute stereocenter assignment is not known.

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

Fmk is an irreversible ribosomal S6 kinase inhibitor 1/2 inhibitor.

Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

CFI-400945 is a potent, highly selective PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM; causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM); significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with mean EC50 of 0.43 nM against a panel of 75 RSV A and B clinical isolates.

Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.

Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme.