Hypocrellin A

SKU: orb1301506

Description

Hypocrellin A is a natural perylenequinone that acts as a protein kinase C (PKC) inhibitor. Its activity is significantly enhanced by light, leading to studied applications in photodynamic therapy for tumors and antimicrobial research. This compound has also been shown to modulate immune responses by affecting MHC-restricted antigen presentation in experimental models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 77029-83-5
• MW: 546.52
• Purity: 99.95%
• Formula: C₃₀H₂₆O₁₀
• SMILES: COc1cc(=O)c2c(O)c(OC)c3CC(C)(O)C(C(C)=O)c4c(OC)c(O)c5c6c(c(OC)cc5=O)c1c2c3c46
• Target: PKC,Parasite,Antibacterial
• Solubility: DMSO:19.23 mg/mL (35.19 mM)

Bioactivity

• Target IC50:
  IL-1β:0.103 μM|HuCCT1 cells proliferation:10.01 μM (24h)|RBE cells proliferation:4.612 μM (24h)|PKC (from soleus muscle):0.26 μg/mL|PKC (from liver):0.07 μg/mL
• In Vivo:
  METHODS: H460 cells were transplanted into athymic female BALB/c nude mice. The mice in the experimental group were intraperitoneally injected with 2.5 mg/kg and 5 mg/kg Hypocrellin A every other day, and the tumor volume of the mice was observed. RESULTS Hypocrellin A reduced NSCLC tumor weight and volume in a concentration-dependent manner.
• In Vitro:
  Method: Three NSCLC cell lines H460, PC-9 and H19755 were treated with 0.01μM, 0.1μM, 0.5μM, 1μM, 5μM, 10μM, 50μM and 100μM HA for 48 hours, and IC50 was determined. RESULTS The IC50 of Hypocrellin A against H1975, H460 and PC-9 were 0.2223μM, 0.2706μM and 0.6223μM respectively. METHODS: A549 cells were collected 12 or 24 h after 24 h treatment with 0.08 μmol/L Hypocrellin A-PDT and apoptosis was measured, aliquots of cell lysates were separated by SDS-PAGE, and lysates were analyzed by Western blotting PARP-1 levels. RESULTS Hypocrellin A-mediated PDT significantly increased the apoptotic population of A549 cells, collectively showing an increase in the proportion of cells in the S phase and G2-M phase, and a decrease in the proportion of cells in the G0-G1 phase, and PARP cleavage in Hypocrellin A begins to occur 3 hours after PDT. METHODS: The isolated tissues of the liver and soleus skeletal muscle parts of the insulin target tissues of obese Zucker rats were treated with Hypocrellin A at concentrations of 0.01, 0.1, 1.0 and 10µg/ml respectively, and the activity of PKC enzyme was measured. RESULTS The IC50 value of Hypocrellin A on liver PKC activity was 0.07µg/ml, and the IC50 value on soleus muscle PKC activity was 0.26µg/ml.
• Cell Research:
  Cells were seeded in 96-well plates at a density of 1*10^4 cells in a final volume of 100 μl and maintained in DMEM medium at 37℃ . After cells were treated with different concentrations of HA (5, 10, 20, 40, 80 μM), 20 μl 5 mg/ml MTT solution were added to each well and incubated for 4 h in the incubator. Then 150 μl DMSO were added to each well to dissolve the pellet, keep it in the dark for 15 min, and dissolve the crystal completely. Automatic microplate reader measured at 490 nm optical density (OD value). The experiment was repeated three times. For combination test, cells were treated with 20 μM Hypocrellin A and different concentrations of OA(25,50,100, 200 μM) .

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

Bacterial, Inhibitor, Hypocrellin A, Parasite, inhibit, PKC, Protein kinase C

Compound Identifiers

PubChem CID

3664