SML1806

YU142670

≥98% (HPLC)

• Synonym(e): 3-(4-pyridinyl)-1,2,4-Triazolo[3,4-b][1,3,4]thiadiazole, 3-(Pyridin-4-yl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
• Empirische Formel (Hill-System): C₈H₅N₅S
• CAS-Nummer: 133847-06-0
• Molekulargewicht: 203.22
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD06590438
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to light brown
• solubility: DMSO: 2 mg/mL, clear (warmed)
• storage temp.: 2-8°C
• SMILES string: C12=NN=C(C3=CC=NC=C3)N1N=CS2
• InChI key: HRBYAJQMVADJHW-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

A selective OCRL1/INPP5F and OCRL2/INPP5B inhibitor that causes cellular PI(4,5)P2 accumulation and autophagosome-lysosome fusion defect.

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.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable