A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.

Desfuroylceftiofur is an active metabolite of Ceftiofur which is a broad-spectrum cephalosporin antibiotic. Desfuroylceftiofur is active against gram-positive and gram-negative bacteria.

NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues.

JNUTS013 is a NLRP3 inflammasome inhibitor. JNUTS013 promotes proteasome-dependent degradation of NLRP3 and inhibits the release of downstream cytokines. JNUTS013 downregulates the expression of inflammation-related proteins including iNOS and COX-2.

(S)-ATPO is the (S)-enantiomer of ATPO, which is a competitive antagonist at GluR1-4 (AMPA-preferring) receptors.

(R)-Ofloxacin is a R-isomer of Ofloxacin, which is an antibiotic useful for the treatment of a number of bacterial infections.

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, is a GABA receptor modulator. It binds to GABAA and GABAB receptors and inhibits GABA uptake in rat brain synaptosomes. (R)-4-amino-3-hydroxybutyric acid is also a GABAC receptor agonist that induces currents in a patch-clamp assay using Xenopus oocytes expressing the human receptor. In vivo, (R)-4-amino-3-hydroxybutyric acid inhibits electrical discharges in the amygdala in a cat model of N-amidinobenzamide-induced seizures.

GSK598809 (GSK-598809) is a potent, selective dopamine D(3) receptor antagonist with Ki value of 6.2 nM, >100-fold selectivity over D2 receptor.

(-)-GSK598809 is an isomer of GSK598809. GSK598809 is a selective D(3)R antagonist recently progressed in Phase I trials. GSK-598809 may decrease the rewarding effects of contextual cues associated with drug intake preclinically, which may reduce drug craving in humans.

NVP-RXI570 is an orally active inhibitors of Brahma Homolog (BRM)/SMARCA2 with IC50 below 0.005 µM.

JM6 (KMO inhibitor JM6) is an orally bioavailable small-molecule prodrug of Ro 61-8048, which is an inhibitor of kynurenine 3-monooxygenase (KMO).

Calcitonin human is an endogenous calcitonin receptor agonist.Calcitonin human lowers systemic blood calcium levels and inhibits bone resorption.

S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.

Novel MmpL3 inhibitor

Novel inhibitor of the heat shock protein 70 (Hsp70) with anti-proliferative activity in breast and prostate cancer cells

SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively.

Dynein2-IN-37 (Ciliobrevin analog 37) is a potent, selective cytoplasmic dynein 2 ATPase activity antagonist with IC50 of 11 uM, shows weak inhibition for dynein 2 (IC50=280 uM).

Syn-TEF1 is a molecule actively enables transcription across repressive GAA repeats that silence frataxin expression in Friedreich's ataxia, license transcription elongation at targeted genomic loci.

DBCO-PEG4-NHS Ester is a PEG derivative containing NHS ester that is able to react specifically and efficiently with primary amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond. The hydrophilic PEG spacer arm improves water solubility and provides a long and flexible connection that minimizes steric hindrance involved with ligation.

OncoACP3 (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 can be used for prostate cancer research.

ACP3 ligand 1 (compound I11a) is a ligand against Acid Phosphatase 3 (ACP3, ACPP). ACP3 ligand 1 interacts with ACP3 expressed on the surface of tumor cells for in vivo pharmaco-delivery applications.

HFI-419 is an insulin-regulated aminopeptidase (IRAP) inhibitor. HFI-419 has inhibitory potency for IRAP with Ki value of 0.48 μM. HFI-419 can be used for the research of cognitive and memory impairments such as Alzheimer's disease, brain trauma, and stroke.

AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice.

NY0128 (NY 0128) is a small molecule neuromedin U receptor 2 (NMUR2) with EC50 of 29.99 uM for hNMUR1 and 10.30 uM for hNMUR2 in intracellular calcium mobilization assays.

NY0116 (NY 0116) is a small molecule neuromedin U receptor 2 (NMUR2) with EC50 of 27.76 uM for hNMUR1 and 13.61 uM for hNMUR2 in intracellular calcium mobilization assays.

A quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine.

RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RASG12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRASG12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer.

Discodermolide (NVP-XAA-296) is a potent microtubule-stabilizing agent with a Ki of 0.4 μM. Discodermolide stabilizes microtubules, induces G2 or M phase cell cycle arrest and apoptosis, leading to inhibition of cancer cell proliferation. Discodermolide competitively inhibits the binding of Paclitaxel to tubulin polymers, and inhibits the growth of Paclitaxel-resistant cells. Discodermolide can be used for breast and colon cancer research.

VTI-1002 is a potent and specific inhibitor of human (K i = 4.4 ± 2.0 nM) and murine (IC 50 = 179 ± 18 nM) GzmB, with minimal activity (IC 50 > 300 nM) against Cathepsin-G, neutrophil elastase and caspases (−3, −4, −5, −7, −8 and −9). In addition to its high specificity for GzmB, VTI-1002 is retained in murine skin for up to 24 hours and exhibits minimal toxicity in vivo with no observed adverse effects after 30 consecutive days of systemic administration in mice [31]. VTI-1002-mediated GzmB inhibition was first reported to augment type I collagen fibrillogenesis and improve tensile strength in a murine diabetic burn model, notably by preventing decorin cleavage and dermal fibrillar collagen network disorganization.

IPA (Inhibitor of Priming Activity) is a small-molecule compound that binds Sec18 (Kd=3.84 uM) and blocks SNARE activation, inhibits vacuole fusion at the SNARE priming stage with IC50 of 50 uM.