Novel Potent Agonist of the Orphan G Protein-Coupled Receptor GPR17 (EC 50 27.9 nM)

Thalidomide-NH-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.

Thalidomide-O-amido-PEG-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.

NUCC-0200590 is a small-molecule inhibitor of the TRIP8b-HCN interaction with IC50 of 7.0 uM in AlphaScreen assays, effectively disrupts the TRIP8b-HCN interaction in vitro and in vivo.

AZD4694, a fluorinated β-amyloid (Aβ) plaque neuroimaging PET radioligand, shows high affinity for Aβ fibrils (Kd = 2.3 nM).

Amino-PEG8-Azido is a non-cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells; PMX-53 (10 nM) inhibited C5a-induced Ca(2+) mobilization in HMC-1 cells, but at higher concentrations (>30 nM) it caused degranulation in LAD2 mast cells, CD34(+) cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2; inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.

Maytansinoid DM4, a chemical derivative of maytansine, is a potent and selective cytotoxic agent with promising anticancer properties. Anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. Maytansin

Pomalidomide 4'-alkylC4-acid (linker 16) is a E3 ligase ligand-linker conjugate. Pomalidomide 4'-alkylC4-acid contains a cereblon ligand, an alkylC4 chain, and a terminal acid. Pomalidomide 4'-alkylC4-acid can be used to couple with target protein ligands to synthesize PROTAC.

(S,R,S)-AHPC-C4-NH2 dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.

D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.

Sodium taurocholate is a GPBAR1 protein agonist potentially for the treatment of type 2 diabetes and obesity in rats.

Novel selective NaV1.7 inhibitor, blocking the extracellular vestibule of the channel with an IC50 of 72 nM and greater than 200-fold selectivity over off-target sodium channel isoforms, NaV1.1-1.6 and NaV1.8

Z218484536 is a selective and brain-penetrant phosphoserine phosphatase (PSPH) inhibitor. Z218484536 binds to PSPH with a Kd value of approximately 0.23 μM. Z218484536 reduces L-serine and D-serine levels in astrocytes. Z218484536 is able to suppress spontaneous epileptic seizures without causing serious side effects. Z218484536 also shows good anti-epileptic effects in the temporal lobe epilepsy (TLE) model.

F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases.

GGACK (H-Glu-Gly-Arg-CMK) hydrochloride is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.

IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy.

FHND5032 is an orally active miR-124 inducer. FHND5032 significantly upregulates miR-124 expression in macrophages. FHND5032 disrupts inflammatory signaling, promotes macrophage reprogramming, and restores the epithelial barrier function by inhibiting the PIK3R2/PI3K/Akt axis. FHND5032 alleviates colitis and reduces inflammatory burden in ulcerative colitis mice. FHND5032 can be used for the study of ulcerative colitis.

7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation and PAR4 signaling pathways, including NF-κB, Ca2+/protein kinase C, Akt, ERK and p38. 7,4'-Dimethoxy-3-hydroxyflavone prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ)-induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time[1][2].

DC-5163 is a potent glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with an IC50 of 176.3 nM and a Kd of 3.192 μM. DC-5163 can inhibit glycolysis pathway partially. DC-5163 also selectively inhibits cancer cell proliferation and induces apoptosis.

α-MSH (11-13) acetate is the 11-13 amino acid (lysine-proline-valine) sequence of α-MSH, which reduces fever in rabbits.