Tyrphostin 8

SKU: orb1694982

Description

Tyrphostin 8 is a GTPase and EGFR kinase inhibitor that also potently inhibits calmodulin-dependent phosphatases. It enhances transferrin receptor-mediated transcytosis in Caco-2 cell models and has been shown to augment the oral hypoglycemic effect of insulin-transferrin conjugates in research studies.

Research Area

Cardiovascular Research, Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 3785-90-8
• MW: 170.17
• Purity: 97.00% (May vary between batches)
• Formula: C₁₀H₆N₂O
• SMILES: OC1=CC=C(C=C(C#N)C#N)C=C1
• Target: Ras,Phosphatase,EGFR,GTPase
• Solubility: DMSO:50 mg/mL (293.82 mM)

Bioactivity

• Target IC50:
  Calcineurin phosphatase:21 μM (IC50)|EGFR:560 μM (IC50)
• In Vivo:
  In Streptozotocin-induced diabetic rats, Tyrphostin 8 enhances the glucose-lowering effect of insulin-transferrin.
• In Vitro:
  Pretreated for 20 minutes at concentrations ranging from 10 to 100 μM, Tyrphostin 8 blocks Carbachol-initiated PKCδ tyrosine phosphorylation and ERK1/2 activation in parotid acinar cells. Additionally, at concentrations of 10-100 μM, Tyrphostin 8 induces a rapid and substantial increase in the basal O2 consumption of parotid acinar cells. Furthermore, at a concentration of 100 μM, Tyrphostin 8 reduces parotid ATP content by approximately 90%. In another context, Tyrphostin 8 enhances the apical-to-basolateral transport of insulin-transferrin conjugate by promoting transferrin receptor-mediated transcytosis in filter-grown Caco-2 cell monolayers.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

4-Hydroxybenzylidenemalononitrile, EGFR, GTPase, Tyrphostin 8

Compound Identifiers

PubChem CID

92970