| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Hypocrellin A targets protein kinase C (PKC) and exerts antitumor effects by inhibiting the FGFR1 signaling pathway in non-small cell lung cancer. It also targets VEGFR, Bcl-2 Family, and apoptosis pathways. As a photosensitizer, it generates reactive oxygen species upon light exposure, which selectively damages target cells.
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| ln Vitro |
In vitro, Hypocrellin A (150 nM; 24 h) significantly reduces the release of VEGF and ET-1 in human umbilical vein endothelial cells (HUVECs) incubated in high glucose (20 mM). It shows good activity against Candida albicans (IC50 = 0.65 µg/ml) and moderate activity against Staphylococcus aureus, MRSA, Pseudomonas aeruginosa, and intracellular mycobacteria. It also exhibits anti-leishmanial activity (IC50 = 0.27 µg/ml).
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| ln Vivo |
In vivo activity data for Hypocrellin A are limited. As a photosensitizer for PDT, it is expected to exhibit antitumor efficacy in animal models upon light activation. Its anti-diabetic activity through reversal of high glucose-induced ET-1 expression suggests potential in vivo effects on diabetic complications.
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| Enzyme Assay |
In vitro enzyme assays for Hypocrellin A are conducted to evaluate PKC inhibition. PKC activity is measured using kinase assay kits with appropriate substrates. FGFR1 inhibition is assessed using kinase assays. Photosensitizing activity is evaluated by measuring reactive oxygen species (ROS) generation upon light activation using fluorescent probes such as DCFH-DA.
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| Cell Assay |
Cellular assays for Hypocrellin A are performed using HUVECs, cancer cell lines, and microbial cultures. Cells are treated with compound concentrations, and VEGF and ET-1 release are measured by ELISA. Antitumor activity is assessed by cell viability assays (MTT, CCK-8) in cancer cell lines. Antimicrobial activity is evaluated by determining minimum inhibitory concentrations (MICs).
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| Animal Protocol |
In vivo animal studies for Hypocrellin A would typically utilize tumor xenograft models for PDT studies. The compound is administered intravenously or intraperitoneally, followed by light irradiation of the tumor site. Endpoints include tumor growth inhibition, survival, and histopathological evaluation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Hypocrellin A are not well characterized. The compound has a molecular weight of 546.52 and a molecular formula of C30H26O10. It is soluble in DMSO (16.67 mg/mL). As a photosensitizer, its tissue distribution and light activation are critical for its efficacy. Standard PK studies in rodents would be required.
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| Toxicity/Toxicokinetics |
Toxicological data for Hypocrellin A are limited. As a photosensitizer, it may cause phototoxicity upon light exposure. No significant acute toxicity has been reported in the absence of light. The compound is designated for research use only.
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| Additional Infomation |
Hypocrellin A is a naphthone compound. Rel-Hypocrellin A has been reported to be detected in bamboo termites (Shiraia bambusicola), and relevant data are available for reference.
Hypocrellin A is a natural PKC inhibitor and photosensitizer with light-induced antitumor, antifungal, and antiviral activities. It exerts antitumor effects by inhibiting the FGFR1 signaling pathway. It shows anti-leishmanial activity (IC50 = 0.27 µg/ml) and activity against Candida albicans (IC50 = 0.65 µg/ml). It has a molecular weight of 546.52 and formula C30H26O10. It is not clinically approved. |
| Molecular Formula |
C30H26O10
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|---|---|
| Molecular Weight |
546.5214
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| Exact Mass |
546.152
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| CAS # |
77029-83-5
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| PubChem CID |
14502645
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| Appearance |
Brown to red solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
894.0±65.0 °C at 760 mmHg
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| Melting Point |
245-250ºC
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| Flash Point |
299.6±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.737
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| LogP |
3.42
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
40
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| Complexity |
1180
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O([H])[C@@]1(C([H])([H])[H])C([H])([H])C2C(=C(C3C(C([H])=C(C4=C5C(=C([H])C(C6C(=C(C(=C(C5=6)C=2C4=3)[C@@]1([H])C(C([H])([H])[H])=O)OC([H])([H])[H])O[H])=O)OC([H])([H])[H])OC([H])([H])[H])=O)O[H])OC([H])([H])[H]
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| InChi Key |
VANSZAOQCMTTPB-RNAHPLFWSA-N
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| InChi Code |
InChI=1S/C30H26O10/c1-10(31)25-24-22-16-11(9-30(25,2)36)28(39-5)26(34)17-12(32)7-14(37-3)19(21(16)17)20-15(38-4)8-13(33)18(23(20)22)27(35)29(24)40-6/h7-8,25,34-36H,9H2,1-6H3/t25-,30+/m1/s1
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| Chemical Name |
(12R,13S)-12-acetyl-9,13,17-trihydroxy-5,10,16,21-tetramethoxy-13-methylhexacyclo[13.8.0.02,11.03,8.04,22.018,23]tricosa-1(15),2(11),3(8),4(22),5,9,16,18(23),20-nonaene-7,19-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~16.67 mg/mL (~30.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.57 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1830 mL | 0.9149 mL | 1.8298 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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