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.
For research use only. We do not sell to patients.
- CAS No.: 366477-44-3
- Formula: C15H15NO3
- Molecular Weight:257.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
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.
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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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Molecular Weight 257.28
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 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
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