H89 · 2HCl

SKU: orb1709506

Description

H-89 is a potent and selective protein kinase A (PKA) inhibitor with an IC50 of 48 nM. It is widely used in cardiovascular research, including studies of myocardial infarction and cardioprotection, and has been shown in rat models to affect spatial learning.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 127243-85-0
• MW: 519.28
• Purity: >98%
• Formula: C₂₀H₂₀BrN₃O₂S·2HCl
• SMILES: O=S(=O)(NCCNCC=CC1=CC=C(Br)C=C1)C2=CC=CC=3C=NC=CC32
• Target: Kinase
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Water (up to 10 mg/ml).

Bioactivity

• Target IC50:
  protein kinase A:48 nM
• In Vivo:
  b>METHODS: H-89 (0.05, 0.1, 0.2 mg/100 g, intraperitoneal injection) was used 30 minutes before the infusion of pentylene tetrazolium (PTZ) in mice to study the effect of H-89 on Bucladesine-induced epileptic activity in PTZ-treated mice. RESULTS: H-89 (0.2 mg/100 g) significantly increased the seizure latency and threshold of PTZ-treated animals; H-89 (0.05, 0.2 mg/100 g) blocked the epileptogenic activity of Bucladesine and significantly increased the seizure latency and seizure threshold.
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• In Vitro:
  Pretreatment of PC12D cells with H-89 (30 μM) significantly inhibited cAMP-dependent histone IIb phosphorylation activity in cell lysates, but did not affect other protein phosphorylation activities ; in rat skin EDL fibers , H-89 (10 μM) only slightly inhibited the force response to depolarization; H-89 (1-2 μM) significantly slowed the re-excitation rate in rat skin EDL fibers, most likely because of its Deleteriously affects the T system potential; H-89 (10-100 μM) also inhibits the net uptake of Ca2+ by SR.
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Storage & Handling

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

Alternative Names

PKA, protein kinase A, Protein kinase inhibitor H-89

Compound Identifiers

PubChem CID

3541