SB-747651A Dihydrochloride

SKU: orb1685257

Description

SB-747651A dihydrochloride is a potent, ATP-competitive MSK1 inhibitor (IC50=11 nM) that also targets PRK2, RSK1, p70S6K, and ROCK-II. This broad kinase inhibition profile makes it a valuable research tool for studying inflammatory signaling pathways in both cellular and animal models of disease.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1781882-72-1
• MW: 415.32
• Purity: 98.05%
• Formula: C₁₆H₂₄Cl₂N₈O
• SMILES: Cl.Cl.CCn1c(nc2cncc(CNC3CCNCC3)c12)-c1nonc1N
• Target: ROCK,p38 MAPK
• Solubility: DMSO:50 mg/mL (120.39 mM)

Bioactivity

• In Vivo:
  SB747651A (3 mg/kg; intrascrotal injection) dihydrochloride significantly increases neutrophil adhesion between 3.5 and 4.5 hours after CXCL2 stimulation . Additionally, the same compound administered intraperitoneally (i.p.) at the same dosage enhances neutrophil extravasation by augmenting neutrophil emigration at the 3 and 4-hour marks in a mouse peritonitis model of acute inflammation . Experiments were conducted on male C57BL/6N mice aged 8 to 16 weeks, confirming that a 3 mg/kg intrascrotal injection results in heightened neutrophil adhesion following CXCL2 stimulation.
• In Vitro:
  SB-747651A dihydrochloride (5 μM; neutrophils) modulates neutrophil behavior in response to the CXCL2 chemotactic gradient by influencing CXCL2-induced intraluminal crawling in a Mac-1-dependent manner, obstructing the movement of adherent neutrophils to optimal emigration sites. It significantly prolongs the transmigration and detachment times of neutrophils, affecting their transendothelial migration. Additionally, it slows the migration velocity of extravascular chemotaxing neutrophils without altering their directionality towards CXCL2 signals.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB 747651A Dihydrochloride, SB-747651A, SB747651A Dihydrochloride, SB-747651A Dihydrochloride, MSK1

Compound Identifiers

PubChem CID

90488958