| Cat. No. |
Product Name |
CAS No. |
Information |
| PC-35278 |
UCB9608
|
1616413-96-7 |
UCB9608 (UCB-9608) is a potent, selective, orally bioavailable PI4KIIIβ inhibitor with IC50 of 11 nM; also shows an IC50 of 37 nM in the human mixed lymphocyte reaction (HuMLR) assay, only inhibits the PI4KIIIβ and PI3KC2 α, β and γ lipid kinases in apnel of 250 kinases tested at 10 uM; UCB9608 is vastly more soluble, selective compound with improved metabolic stability and excellent pharmacokinetic profile, significantly prolongs allogeneic organ engraftment in vivo.
|
| PC-61695 |
BQR-695
|
1513879-21-4 |
BQR-695 (NVP-BQR695) is a highly potent, selective PI4KIIIβ inhibitor that has high potency against both the human (IC50 = 80 nM) and PvPI4K (IC50=3.5 nM) ; shows >100 fold more potent over all other class I and class III PI3K isoforms; induces a schizont-stage arrest in imidazopyrazine-treated parasites and exhibits cross-resistance with the imidazopyrazine-resistant lines; a novel antimalarial compound that inhibits the intracellular development of multiple Plasmodium species at each stage of infection in the vertebrate host.
|
| PC-61691 |
MMV390048
|
1314883-11-8 |
MMV390048 is a novel potent Plasmodium PI4K inhibitor with IC50 of 28 nM against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain); blocks all life cycle stages of the malaria parasite, exhibits full chemoprotection, delays relapse in a Plasmodium cynomolgi monkey model.
Parasite Infection
Phase 2 Clinical
|
| PC-61327 |
PI-273
|
925069-34-7 |
PI-273 (PI273) is a potent, specific, substrate-competitive small molecule inhibitor of PI4KIIα with IC50 of 0.47 uM; reduces PI4P content, cell viability and AKT signaling in wild-type MCF-7 cells but not in PI4KIIα knockout MCF-7 cells; retards cell proliferation by blocking cells in G2/M, inducing cell apoptosis and suppressing colony-forming ability, significantly inhibits MCF-7 cell-induced breast tumor growth without toxicity in a xenograft model (intravenous or intragastrical).
|
| PC-35292 |
UCT943
|
1450666-80-4 |
UCT943 (UCT-943) is a potent, selective, next generation Plasmodium falciparum PI4K inhibitor with IC50 of 23 nM; displays higher asexual blood stage, transmission-blocking, and liver stage activity than MMV048 and is more potent against resistant P. falciparum and P. vivax clinical isolates; demonstrates excellent in vitro antiplasmodial activity in P. berghei and humanized P. falciparum mouse models. |
| PC-35202 |
PI4KA inhibitor A1
|
1416334-69-4 |
PI4KA inhibitor A1 (GSK-A1) is a highly specific and potent inhibitor of PI4KA. |
| PC-42861 |
PIK-93
|
593960-11-3 |
PIK-93 is a potent, synthetic PI4K inhibitor with IC50 of 19 nM (PI4KIIIβ), also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively; also inhibits other PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 uM, and 0.12 uM, shows no inhibitory effect against a panel of other kinases; significantly inhibits the conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin, reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry in T6.11 cells at 300 nM; also demonstrates anti-enterovirus effects by inhibition of both poliovirus and HCV replication with EC50 of 0.14 uM and 1.9 uM, respectively. |
