PIK-93

SKU: orb1224543

Description

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.

Key Properties

• CAS Number: 593960-11-3
• MW: 389.8775
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₆ClN₃O₄S₂
• SMILES: CC(NC1=NC(C)=C(C2=CC=C(Cl)C(S(=O)(NCCO)=O)=C2)S1)=O
• Target: PI4K
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC50 values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC50 values of 39 nM, 0.59 μM, and 0.12 μM, respectively. PIK-93 shows no obvious inhibitory effect against a panel of other kinases, even at a concentration of 10 μM. In differentiated HL60 (dHL60) cells, PIK-93 (0.5 μM-1 μM) impairs consolidation and stability of the leading edge formed after treatment with uniform f-Met-Leu-Phe (fMLP). PIK-93 alters the localization, but not the amount, of the fMLP-dependent accumulation of total F-actin. In fMLP gradients, PIK-93 reduces the chemotactic index and triples the cells' turning frequency. In COS-7 cells, PIK-93 (250 nM) effectively abrogates the accumulation of CERT-PH domain and FL-Cer in Golgi. PIK-93 of the same concentration also significantly inhibits the conversion of [3H]serine-labeled endogenous ceramide to sphingomyelin. These facts indicate a key role of PI4KIIIβ in ceramide transport between the ER and Golgi, as well as in the regulation of spingomyelin synthesis. In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca2+ entry. A recent report shows that PIK-93 has anti-enterovirus effects, as revealed by its inhibition of both poliovirus (PV) and hepatitis C virus (HCV) replication, with EC50 values of 0.14 μM and 1.9 μM, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PIK 93 | PIK93

Quick Database Links

Gene Symbol

PI4K