BQR-695

Research use only, not for human use.

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).

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.

Treatment with 0.5 μM of either KAI407 or BQR695 causes GFP-PHOsh2 to redistribute to the parasite plasma membrane, consistent with depletion of intracellular PI4P upon inhibition of PfPI4K function. BQR695 shows no evidence of toxicity against mature red blood cells (RBCs), induces a schizont-stage arrest indistinguishable from that observed in imidazopyrazine-treated parasites and exhibits cross-resistance with the imidazopyrazine-resistant lines.

——

BQR695 | NVP-BQR695

PI3K/Akt/mTOR signaling

PI4K

PI3KIIIβ|PI4KIIIβ

——

——

1513879-21-4

352.394

C19H20N4O3

>98% (HPLC)

DMSO: 100 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(NC)CNC1=NC2=CC(C3=CC=C(OC)C(OC)=C3)=CC=C2N=C1

2-[[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]amino]-N-methylacetamide

(-20℃)

With Ice Pack

≥ 2 years