[CAS NO. 593960-11-3] PIK-93
PRODUCTS SPECIFICATIONS [593960-11-3]
DESCRIPTION [593960-11-3]
Overview
| MDL | MFCD12922510 |
|---|---|
| Molecular Weight | 389.88 |
| Molecular Formula | C14H16ClN3O4S2 |
| SMILES | CC(NC1=NC(C)=C(S1)C2=CC=C(C(S(=O)(NCCO)=O)=C2)Cl)=O |
5 Publications Citing Use of MCE
Summary
IC50 & Target
|
PI4KIIIβ 19 nM (IC 50 ) |
PI4KIIIα 1.1 μM (IC 50 ) |
p110γ 16 nM (IC 50 ) |
p110α 39 nM (IC 50 ) |
p110δ 120 nM (IC 50 ) |
p110β 590 nM (IC 50 ) |
PI3KC2β 140 nM (IC 50 ) |
|
|
PI3KC2α 16 μM (IC 50 ) |
hsVPS34 320 nM (IC 50 ) |
DNA-PK 64 nM (IC 50 ) |
ATM 490 nM (IC 50 ) |
mTORC1 1.38 μM (IC 50 ) |
ATR 17 μM (IC 50 ) |
||
In Vitro
PIK-93 inhibits PI3Kγ and PI4KIIIβ, with IC 50 values of 16 nM and 19 nM, respectively. PIK-93 also inhibits other members of PI3Ks, including PI3Kα, β, and δ, with IC 50 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 [1] . 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 [2] . 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 [ 3 H]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 [3] . In T6.11 cells, PIK-93 (300 nM) reduces carbachol-induced translocation of TRPC6 to the plasma membrane and net Ca 2+ entry [4] . 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 EC 50 values of 0.14 µM and 1.9 µM, respectively [5] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 256.49 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5649 mL | 12.8245 mL | 25.6489 mL |
| 5 mM | 0.5130 mL | 2.5649 mL | 5.1298 mL |
| 10 mM | 0.2565 mL | 1.2824 mL | 2.5649 mL |
References
- [1] Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47
- [2] Van Keymeulen A, et al. To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front. J Cell Biol. 2006 Jul 31;174(3):437-45
- [3] Toth B, et al. Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi. J Biol Chem. 2006 Nov 24;281(47):36369-77
- [4] Monet M, et al. Involvement of phosphoinositide 3-kinase and PTEN protein in mechanism of activation of TRPC6 protein in vascular smooth muscle cells. J Biol Chem. 2012 May 18;287(21):17672-81
- [5] Arita M, et al. Phosphatidylinositol 4-kinase III beta is a target of enviroxime-like compounds for antipoliovirus activity. J Virol. 2011 Mar;85(5):2364-72