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Key Documents

SML1806

Sigma-Aldrich

YU142670

≥98% (HPLC)

Synonym(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

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About This Item

Empirical Formula (Hill Notation):
C8H5N5S
CAS Number:
Molecular Weight:
203.22
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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