BLU0588

SKU: orb1819253

Description

BLU0588 is a potent and selective inhibitor of PRKACA catalytic activity, exhibiting an IC50 of 1 nM. This small molecule is a valuable research tool for investigating cAMP-dependent signaling pathways in both cellular and biochemical assays.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2810747-78-3
• MW: 423.51
• Purity: 99.85% (May vary between batches)
• Formula: C₂₆H₂₅N₅O
• SMILES: O=C(N[C@@H]1C2=C(C=CC=C2)C[C@H]1N1CCCC1)C1=CC=C(C2=C3C=CNC3=NC=C2)N=C1
• Target: Others,PKA
• Solubility: DMSO:85.8 mg/mL (202.59 mM)

Bioactivity

• Target IC50:
  RKACA (PHOS cellsphorylation of VASP Ser157 in Huh7 cells):25.0 nM|PRKACA:4 nM (Kd)|PRKACA:1 nM
• In Vivo:
  For in vivo studies, mice were given either BLU0588 at 30 mg/kg and 75 mg/kg once daily (QD) and monitored for 24 hours. Plasma concentrations peaked within 2–4 hours of QD dosing. For BLU0588-treated mice, phosphorylated VASP was reduced to 19% and 4% of baseline phosphorylation levels with 30 mg/kg QD and 75 mg/kg QD, respectively, 4 hours after dosing; phosphorylated VASP levels fully recovered by 24 hours post administration of 30 mg/kg QD. When mice harboring FLC PDX tumors were treated with BLU0588 given orally at 30 mg/kg QD, by Day 34 tumor growth was inhibited by 48.5% (P = 0.003).
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• In Vitro:
  RKACA cellular IC50 values were 25.0 nM with BLU0588, which were determined from inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells.
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Storage & Handling

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

Alternative Names

PRKACA, BLU0588, BLU-0588, BLU 0588

Compound Identifiers

PubChem CID

164603520