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SML1806

Sigma-Aldrich

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

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About This Item

Empirische Formel (Hill-System):
C8H5N5S
CAS-Nummer:
133847-06-0
Molekulargewicht:
203.22
MDL-Nummer:
MFCD06590438
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to light brown

Löslichkeit

DMSO: 2 mg/mL, clear (warmed)

Lagertemp.

2-8°C

SMILES String

C12=NN=C(C3=CC=NC=C3)N1N=CS2

Biochem./physiol. Wirkung

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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Maria Giovanna De Leo et al.
Nature cell biology, 18(8), 839-850 (2016-07-12)
Phosphoinositides (PtdIns) control fundamental cell processes, and inherited defects of PtdIns kinases or phosphatases cause severe human diseases, including Lowe syndrome due to mutations in OCRL, which encodes a PtdIns(4,5)P2 5-phosphatase. Here we unveil a lysosomal response to the arrival
Michelle Pirruccello et al.
ACS chemical biology, 9(6), 1359-1368 (2014-04-20)
Phosphoinositides are low abundance membrane phospholipids that have key roles in signaling, membrane trafficking, and cytoskeletal dynamics in all cells. Until recently, strategies for robust and quantitative development of pharmacological tools for manipulating phosphoinositide levels have focused selectively on PI(3,4,5)P3
Stephen J Mills et al.
Biochemistry, 55(9), 1384-1397 (2016-02-09)
The inositol polyphosphate 5-phosphatase INPP5B hydrolyzes the 5-phosphate group from water- and lipid-soluble signaling messengers. Two synthetic benzene and biphenyl polyphosphates (BzP/BiPhPs), simplified surrogates of inositol phosphates and phospholipid headgroups, were identified by thermodynamic studies as potent INPP5B ligands. The

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