An activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells

Vacquinol-1 – 5 mg

Brand:
Cayman
CAS:
5428-80-8
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Vacquinols are a new class of quinine-derivatives that stimulate death in glioblastoma cells by massive macropinocytotic vacuolization, ATP depletion, and cytoplasmic membrane rupture.{26440} A key effector of vacquinols is MAPK kinase 4 (MKK4).{26440} Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.{26440} It induces ATP depletion in glioblastoma cells (IC50 = 3.14 µM at 1 day) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells.{26440} Vacquinol-1 is orally bioavailable with good brain penetrance and excellent pharmacokinetics.{26440} Oral administration of vacquinol-1 (20 mg/kg once daily for five days) substantially impairs the growth of engrafted glioblastoma cell tumors in mice and prolongs survival.{26440}  

 

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Description

An activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells, inducing ATP depletion (IC50 = 3.14 µM at 1 day); orally bioavailable, substantially impairing the growth of engrafted glioblastoma cell tumors in mice

Formal name: 2-(4-chlorophenyl)-α-2-piperidinyl-4-quinolinemethanol

Synonyms:  NSC 13316

Molecular weight: 352.9

CAS: 5428-80-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Kinases||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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