Haplophytin-A
Based on 1 Customer Validation
Haplophytin-A is a quinoline alkaloid. Haplophytin-A is a potent apoptosis inducer that exerts robust anti-leukemic activity by activating the caspase-8-dependent apoptotic pathway. Haplophytin-A can be used for the research of promyelocytic leukemia.
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- CAS No.: 366477-44-3
- Formule: C15H15NO3
- Masse moléculaire:257.28
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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Caspase 8 |
Caspase 3 |
Caspase 9 |
Bcl-2 |
Bcl-xL |
In Vitro
Haplophytin-A (48 h) induces cytotoxicity in human cancer cell lines, with the highest potency against HL-60 promyelocytic leukemia cells (IC50 = 13.7 μM)[1].
Haplophytin-A (15-50 μM; 0-6 h) induces apoptosis in HL-60 cells, as shown by time- and dose-dependent DNA fragmentation and increased Annexin V-positive cells[1].
Haplophytin-A (50 μM; 0-6 h) activates caspase-8, caspase-9, caspase-3, and cleaves PARP in HL-60 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:human promyelocytic leukemia HL-60 cells
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Concentration:15, 30 and 50 μM
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Incubation Time:0, 1, 2, 4 and 6 h
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Result:Caused time- and dose-dependent DNA fragmentation, with ~70% fragmentation observed at 50 μM for 6 h.
Produced a DNA ladder pattern at 4 h with 50 μM.
Increased Annexin V-positive cells to 42.29% after 6 h with 50 μM.
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Cell Line:human promyelocytic leukemia HL-60 cells
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Concentration:50 μM
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Incubation Time:0, 1, 2, 4 and 6 h
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Result:Activated caspase-8 and -9 at 2 h, and caspase-3 and cleaved PARP at 4 h.
Was blocked from inducing DNA fragmentation at 50 μM for 6 h when co-treated with caspase inhibitors (z-DEVD-fmk, z-IETD-fmk, z-LEHD-fmk, z-VAD-fmk).\n
Induced Fas-FasL interaction at 1 h and FADD-procaspase-8 association at 2 h, forming the Fas-FasL-FADD-caspase-8 DISC complex.
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Cell Line:human promyelocytic leukemia HL-60 cells
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Concentration:50 μM; 50 μM (with 5 μM CsA pretreatment for 30 min)
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Incubation Time:0, 1, 2, 4 and 6 h
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Result:Reduced cytosolic Bid/Bax and increased mitochondrial Bid/Bax.
Decreased Bcl-2/Bcl-XL levels, reduced Δψₘ (attenuated by CsA), and induced cytochrome c/Smac/DIABLO release to cytosol.
Increased Smac/DIABLO-XIAP interaction and dissociated XIAP from procaspase-9/-3.
Chemical Information
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CAS No. 366477-44-3
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Appearance Solid
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Masse moléculaire 257.28
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Formule C15H15NO3
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SMILES
O=C1NC2=C(C(OC)=CC=C2)C3=C1C=CC(C)(C)O3
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (388.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureté et documentation
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Fiche technique (281 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Won KJ, et al. Haplophytin-A induces caspase-8-mediated apoptosis via the formation of death-inducing signaling complex in human promyelocytic leukemia HL-60 cells. Chem Biol Interact. 2010;188(3):505-511. [Content Brief]
[2]. Ali MS, et al. Haplophytin-A and B: the alkaloidal constituents of Haplophyllum acutifolium. Phytochemistry. 2001;57(8):1277-1280. [Content Brief]
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 |
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| DMSO | 1 mM | 3.8868 mL | 19.4341 mL | 38.8682 mL | 97.1704 mL |
| 5 mM | 0.7774 mL | 3.8868 mL | 7.7736 mL | 19.4341 mL | |
| 10 mM | 0.3887 mL | 1.9434 mL | 3.8868 mL | 9.7170 mL | |
| 15 mM | 0.2591 mL | 1.2956 mL | 2.5912 mL | 6.4780 mL | |
| 20 mM | 0.1943 mL | 0.9717 mL | 1.9434 mL | 4.8585 mL | |
| 25 mM | 0.1555 mL | 0.7774 mL | 1.5547 mL | 3.8868 mL | |
| 30 mM | 0.1296 mL | 0.6478 mL | 1.2956 mL | 3.2390 mL | |
| 40 mM | 0.0972 mL | 0.4859 mL | 0.9717 mL | 2.4293 mL | |
| 50 mM | 0.0777 mL | 0.3887 mL | 0.7774 mL | 1.9434 mL | |
| 60 mM | 0.0648 mL | 0.3239 mL | 0.6478 mL | 1.6195 mL | |
| 80 mM | 0.0486 mL | 0.2429 mL | 0.4859 mL | 1.2146 mL | |
| 100 mM | 0.0389 mL | 0.1943 mL | 0.3887 mL | 0.9717 mL |
Haplophytin-A Related Classifications
HY-N17612 Related Classifications
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