Biochem/physiol Actions
YU142670 is a selective inhibitor against OCRL1/INPP5F (IC50 = 0.71 µM; substrate = PI(4,5)P2) and OCRL2/INPP5B (IC50 = 0.53 and 1.78 µM; substrate = PI3 and INPP5B/PI(4,5)P2, respectively) by targeting OCRL catalytic domain without affecting INPP5A, INPP5E, PTEN, SHP1, shrimp alkaline phosphatase, sphingomyelinase, or SYNJ1. YU142670 causes an increased PI(4,5)P2/PI4P ratio in human skin fibroblasts (by 50%; 50 µM for 1 h) and induces upregulated actin nucleation and ruffle activity at the plasma membrane without obvious cytotoxicity. Consistent with the negative regulatory role of PtdIns(4,5)P2 against the calcium channel mucolipin-1 (MCOLN1) that controls autophagosome-lysosome fusion, ehnahced autophagosome accumulation is observed in human kidney proximal tubule cells (PTCs) upon YU142670 (25 µM for 3 hr) or OCRL shRNA treatment.
Packaging
5, 25 mg in glass bottle
| Colour | white to light brown |
|---|---|
| Quality Level | 100 |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | 2-8°C |
| Solubility | DMSO: 2 mg/mL, clear (warmed) |
| Form | powder |
| Assay | ≥98% (HPLC) |
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