DPQ (also known as PARP Inhibitor III) is a novel and potent inhibitor of PARPs [The poly(ADP-ribose) polymerases] which inhibits PARP1 activity with an IC50 value of 40 nM. It is approximately 10-fold less potent against PARP2. DPQ can be used in either cells or in animals. The poly(ADP-ribose) polymerases (PARPs) form a family of […]

Furathiocarb is a carbamate pesticide

PF-06821497 (PF06821497) is a novel, potent, selective and orally bioactive Enhancer of Zeste Homolog 2 (EZH2) inhibitor with potential anticancer effects. It inhibits EZH2 with a Ki value

24, 25-Dihydroxy Vitamin D3 (24, 25-Dihydroxy D3; 24, 25-Dihydroxy VD3) is a vitamin D3 analog with important biological activities (anticancer, antiinflammatory et al.). It is closely related to 1,25-dihydroxyvitamin D3 (the active form of vitamin D3), but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo.

UNC4976 is a significantly improved cellularly efficacious chemical probe of CBX7. UNC4976 acts as a positive allosteric modulator (PAM) of CBX7 chromodomain binding to nucleic acids with rapid impacts on both PRC1 occupancy on chromatin and gene expression at Polycomb target genes within cells. UNC4976 results enhanced efficacy across three orthogonal cellular assays by simultaneously […]

CP-10 (CP10; CP 10), designed from a focused PROTAC library hijacking cancer therapeutic target CDK6, is a novel and potent PROTAC-based protein degrader targeting CDK6 with high selectivity, specificity, and remarkable CDK6 degradation efficiency (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated […]

Elenbecestat (E-2609; E2609) is a novel, potent orally bioactive and BBB-penetrant BACE1 inhibitor which can reduce the plasma beta-amyloid levels after single dosing and has the potential for the treatment of Alzheimer’s disease (AD). By inhibiting BACE, a key enzyme in the production of Aβ peptides, E2609 decreases the formation of these peptides which can […]

Ornoprostil (OU-1308), a methyl derivative of PGE1 developed in Japan, is a prostaglandin E1 analogue that acts as a mucosal protectant. Ornoprostil protects gastric mucosa against damage caused by concentrated ethanol.

PI3Kδ inhibitor 2 is a novel, highly potent and selective PI3Kδ inhibitor with IC50 of 0.9 nM in the enzyme assay, and 20-120nM of cell potency in a JeKo-cell assay. It exhibits a high selectivity (>1000-fold) over PI3K isoforms such as PI3Kα, PI3Kβ, PI3Kγ (IC50>1.5 uM). It has reasonable pharmacokinetic properties such as good bioavailability […]

Lanraplenib (also known as GS-9876; GS-SYK) is a highly selective and orally bioavailable Spleen Tyrosine Kinase (SYK) inhibitor with IC50 of 9.5 nM). It is currently under development by Gilead for the treatment of inflammatory diseases such as RA. Spleen Tyrosine Kinase (SYK) mediates signaling in a range of hematopoietic cells involved in the initiation […]