R 59-022 hydrochloride

SKU: orb2900570

Description

R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 μM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

Key Properties

• CAS Number: 93076-98-3
• MW: 496.04
• Purity: >98% (HPLC)
• 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
• Solubility: In Vitro: DMSO : 25 mg/mL (50.40 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Animal model: SCID mice implanted with U87 GBM cells. Dosage: 10 mg/kg. Administration: Intraperitoneal injection (i.p.). Result: Increased median survival and decreased tumor volume.
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• In Vitro:
  Western blot analysis. Cell line: HeLa cells. Concentration: 40 uM. Incubation time: 30 min. Result: Increased the phosphorylation of PKC downstream targets by about 2.5-fold.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PKC