PI4K|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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The phosphatidylinositol 4-kinases (PI4Ks) synthesize phosphatidylinositol 4-phosphate (PI4P), a key member of the phosphoinositide family. PI4P defines the membranes of Golgi and trans-Golgi network (TGN) and regulates trafficking to and from the Golgi.

In mammals there are four different PI4K enzymes, two type II enzymes (PI4KIIα and PI4KIIβ) and two type III enzymes (PI4KIIIα and PI4KIIIβ). PI4KIIIβ plays key roles in mediating lipid transport, cytokinesis, maintaining lysosomal identity, and in tandem with Rab GTPases plays key roles in regulating membrane trafficking. PI4KIIIβ is critical for mediating viral replication of a number of RNA viruses through the generation of PI4P enriched viral replication platforms. Small molecule inhibitors of PI4KIIIβ are potent anti-viral agents. Development of PI4KIIIβ as an effective drug target for anti-viral therapeutics requires the generation of highly potent and specific inhibitors.

Cat. No.	Product Name	CAS No.	Information
H7106	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.
H7105	PI4KIIIβ-IN-9	1429624-84-9	PI4KIIIβ-IN-9 is a potent and selective inhibitor of PI4KIIIβ (IC50=7 nM); displays >1000-fold selectivity over class I and class III PI3Ks; A KN-93 derivative with improved selectivity.
H7104	PI4KIIIbeta-IN-10	1881233-39-1	A potent and selective type III phosphatidylinositol 4-kinase (PI4KIIIβ) inhibitor with IC50 of 3.6 nM; displays >200-fold selectivity over class I and class III PI3Ks; shows antiviral activity against hepatitis C virus with IC50 of 1.3 uM, with low cytotoxicity (CC50>32 uM).
H7103	PI4KA inhibitor A1	1416334-69-4	PI4KA inhibitor A1 (GSK-A1) is a highly specific and potent inhibitor of PI4KA.
H7102	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).
H7101	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.
H7100	KDU731	1610610-48-4	KDU731 is a potent, selective parasite Cryptosporidium lipid kinase PI4K (phosphatidylinositol-4-OH kinase) inhibitor with IC50 of 25 nM, displays >50-fold selectivity window against the human PI4K IIIβ homologue; shows HepG2 CC50 of 15.6 uM and C. parvum CPE EC50 of 0.1 uM; demonstrates a potent reduction in intestinal infection of immunocompromised mice after oral treatment, also leads to rapid resolution of diarrhoea and dehydration in neonatal calves, a clinical model of cryptosporidiosis that closely resembles human infection.
H7099	KDU-691	1513879-19-0	KDU-691 is a potent, selective, orally active parasite PI4K inhibitor with IC50 of 1.5 nM for P. vivax PI4K (PvPI4K); shows IC50 of 58 nM, 36 nM and 196 nM against P. falciparum (Pf, boold stages), P. yoelii (Py, schizont) and P. cynomolgi (Pc, hypnozoites) respectively; shows fully protective effect against P. cynomolgi sporozoites in animal models.
H7098	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.
H7108	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.

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