R 59-022 hydrochloride

SKU: orb1744976

Description

R 59-022 hydrochloride is a diacylglycerol kinase (DGK) inhibitor (IC50: 2.8 µM) and 5-HT receptor antagonist that activates PKC. It is used in research to modulate lipid signaling, such as enhancing thrombin-induced diglyceride production in platelets and inhibiting phosphatidic acid formation in neutrophils.

Research Area

Epigenetics & Chromatin, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 93076-98-3
• MW: 496.04
• Purity: 98.33%
• Formula: C₂₇H₂₇ClFN₃OS
• SMILES: Cl.O=C1C(=C(N=C2SC=CN21)C)CCN3CCC(=C(C=4C=CC=CC4)C5=CC=C(F)C=C5)CC3
• Target: PKC,5-HT Receptor
• Solubility: DMSO:55 mg/mL (110.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.03 mM)

Bioactivity

• Target IC50:
  DGK:2.8 µM
• In Vivo:
  R 59-022 (2 mg/kg; i.p.; 12 days) significantly increased the median survival of SCID mice implanted with U87 GBM cells.
• In Vitro:
  R 59-022 (10 μM; 1 min) Hydrochloride enhances platelet aggregation. R 59-022 (30 μM; 0-60 min) Hydrochloride increases the release of norepinephrine in chromaffin cells. R 59-022 (40 μM; 30 min) Hydrochloride activates PKC in HeLa and U87 cells. R 59-022 (0-10 μM; 4 h) Hydrochloride blocks the entry of EBOV GP into Vero cells.

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

R 59-022 Hydrochloride, PKC, 5HTReceptor, 5HT Receptor, 5-HT Receptor, DKGI-I Hydrochloride, DKGI-I hydrochloride, DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride, Diacylglycerol kinase inhibitor I Hydrochloride, Diacylglycerol kinase inhibitor I hydrochloride, DGK

Compound Identifiers

PubChem CID

23326062