1. Epigenetics TGF-beta/Smad Anti-infection Protein Tyrosine Kinase/RTK Apoptosis
  2. PKC Bacterial Parasite HIV VSV VEGFR Bcl-2 Family Apoptosis
  3. Hypocrellin A

Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml).

For research use only. We do not sell to patients.

Hypocrellin A Chemical Structure

Hypocrellin A Chemical Structure

CAS No. : 77029-83-5

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Based on 1 publication(s) in Google Scholar

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  • Purity & Documentation

  • References

  • Customer Review

Description

Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].

IC50 & Target

Leishmania

 

In Vitro

Hypocrellin A (150 nM; 24 h) significantly reduces the release of VEGF and ET-1 from human umbilical vein endothelial cells (HUVECs) incubated in glucose (20 mM)[1].
Hypocrellin A shows good activity against Candida albicans (IC50=0.65 μg/ml) and moderates activity against Staphylococcus aureus, MRSA, Pseudomonas aeruginosa, and Mycobacterium intracellularis[4].
Hypocrellin A (0.055-5.5 µM) loses the infectivity of both HIV-1 and VSV in a concentration-dependent manner when treats with 1 J/cm2 white light[5].
Hypocrellin A (5 µM; 6 h) increases the secretion of multiple anti-angiogenic factors in LN229 glioma, U937 macrophages and SVHCEC endothelial cells after photochemotherapy[6].
Hypocrellin A (0.25-1 µM; 48 h) has a negative impact on cell viability, migration, invasion and apoptosis of three non-small cell lung cancer cells, H460, PC-9 and H1975[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs) incubated in glucose (20 mM)
Concentration: 150 nM
Incubation Time: 24 h
Result: Reduced VEGF protein expression.

Western Blot Analysis[6]

Cell Line: LN229 glioma, U937 macrophages, and SVHCEC endothelial cells
Concentration: 5 µM
Incubation Time: 6 h
Result: Induced production of roangiogenic VEGF (vascular endothelial growth factor) and of antiangiogenic sFlt-1, angiostatin, p43, allograft inflammatory factor-1, and connective tissue growth factor.

Cell Viability Assay[8]

Cell Line: H460, PC-9 and H1975 cell lines
Concentration: 0.25, 0.5 and 1 µM
Incubation Time: 48 h
Result: The IC50 values for H460, PC-9 and H1975 cell lines were 0.2706, 0.6223 and 0.2223 µM, respectively.

Western Blot Analysis[8]

Cell Line: H460, PC-9 and H1975 cell lines
Concentration: 0.25, 0.5 and 1 µM
Incubation Time: 48 h
Result: Increased the expression levels of pro-apoptotic proteins BAX and Cl-PARP, and decreased the expression level of anti-apoptotic protein BCL-2.
In Vivo

Hypocrellin A (2.5 and 5 mg/kg; i.p.; once every two days for fourteen days) inhibits tumor growth in a non-small cell lung cancer xenograft model mouse model[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: H460 cells were inoculated subcutaneously on the backs of BALB/c nude mice[8]
Dosage: 2.5 and 5 mg/kg
Administration: i.p.; Inject once every two days for fourteen days
Result: Induced the expression of the pro-apoptotic protein BAX and inhibited the expression of the anti-apoptotic protein BCL-2 in NSCLC tumors.
Molecular Weight

546.52

Formula

C30H26O10

CAS No.
Appearance

Solid

Color

Brown to red

SMILES

COC(C1=O)=C2C3=C(C1=C(C=C4OC)O)C4=C(C(OC)=CC(O)=C56)C5=C3C(CC(C)(O)C2C(C)=O)=C(OC)C6=O

Structure Classification
Initial Source

Shiraia bambusicola

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (30.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8298 mL 9.1488 mL 18.2976 mL
5 mM 0.3660 mL 1.8298 mL 3.6595 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.57 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.73%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8298 mL 9.1488 mL 18.2976 mL 45.7440 mL
5 mM 0.3660 mL 1.8298 mL 3.6595 mL 9.1488 mL
10 mM 0.1830 mL 0.9149 mL 1.8298 mL 4.5744 mL
15 mM 0.1220 mL 0.6099 mL 1.2198 mL 3.0496 mL
20 mM 0.0915 mL 0.4574 mL 0.9149 mL 2.2872 mL
25 mM 0.0732 mL 0.3660 mL 0.7319 mL 1.8298 mL
30 mM 0.0610 mL 0.3050 mL 0.6099 mL 1.5248 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Hypocrellin A
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