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PIK-93 is a PI4KIIIβ inhibitor (IC50 at 19 nM). PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range. In addition, this compound also inhibits potently PI3Kγ in vitro (IC50 at 16 nM). This compound inhibits p110α, p110β, p110δwith IC50 of 0.039, 0.59, 0.12 µM. PIK-93 also displays the typical hydrogen bonding to the backbone amide of Val882, and additional ones to the backbone carbonyl of Val882 and between its sulphonamide and Asp964.
| Cell Experiment | |
|---|---|
| Cell lines | Differentiated HL60 (dHL60) cells |
| Preparation method | For actin staining, preincubate dHL60 cells in suspension with PIK-93 or vehicle for 40 min, centrifuge for 5 min at 2000 rpm at room temperature in a J6-B centrifuge, resuspend in mHBSS containing the respective agent at the same concentration, allowed to stick to fibronectin-covered coverslips, and subject to stimulation with a uniform concentration of 100 nM f-Met-Leu-Phe (fMLP) for 3 min. Fixing cellsare in 3.7% PFA and staining with 10 units/mL rhodamine-phalloidin for 15 min |
| Concentrations | 0.5 μM–1 μM |
| Incubation time | 40 min |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 389.88 |
| Formula | C14H16ClN3O4S2 |
| CAS Number | 593960-11-3 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Wendy Zhang, et al. Mitigating Motor Neuronal Loss in C. elegans Model of ALS8
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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