SML1806

YU142670

≥98% (HPLC)

• Synonyme(s) : 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
• Formule empirique (notation de Hill) : C₈H₅N₅S
• CAS Number: 133847-06-0
• Poids moléculaire : 203.22
• Numéro MDL: MFCD06590438
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to light brown
• Solubilité: DMSO: 2 mg/mL, clear (warmed)
• Température de stockage: 2-8°C
• Chaîne SMILES: C12=NN=C(C3=CC=NC=C3)N1N=CS2
• Clé InChI: HRBYAJQMVADJHW-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable