WHN-11
WHN-11 is an amino-Artemisinin (HY-B0094) derivative with anti-cancer activity against various cancer cell lines. WHN-11 deprives the cell of ATP, activates autophagy, and causes subsequent cell death by apoptosis. WHN-11 alters cellular protein homeostasis pathways to induce mitochondrial fission and dysfunction. WHN-11's anti-cancer activity is independent of substantive ROS production. WHN-11 can be used for the study of triple-negative breast cancer (TNBC).
For research use only. We do not sell to patients.
- Formula: C27H36F3N3O5
- Molecular Weight:539.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
15 μM
Compound: 9i
|
Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
| A549 | IC50 |
21.1 μM
Compound: 9i
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
| L02 | IC50 |
4 μM
Compound: 9i
|
Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
| MCF7 | IC50 |
2.7 μM
Compound: 9i
|
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
| MDA-MB-231 | IC50 |
5.8 μM
Compound: 9i
|
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
| SH-SY5Y | IC50 |
3.2 μM
Compound: 9i
|
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
| U-87MG ATCC | IC50 |
15.2 μM
Compound: 9i
|
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 29789258] |
In Vitro
WHN-11 exhibits significant cytotoxicity against HCC1937 (IC50 = 0.74 μM), HCC70 (0.19 μM) and MDA-MB-231 TNBC cell lines (0.5 μM), HeLa cervical carcinoma (0.84 μM), U87 glioblastoma (6.57 μM), 501mel melanoma (0.2 μM) and HCT116 colon cancer cell lines (0.44 μM)[1].
WHN-11 inhibits tumoursphere formation in the HCC1937 TNBC cell line[1].
WHN-11 (5-80 μM, 9 days) significantly decreases colony formation of HCC1937 cells in a dose-dependent manner[1].
WHN-11 (1-50 μM, 24 h) promotes the cleavage of caspase-3 in a dose-dependent fashion rather than RARP-1[1].
WHN-11 does not alter ROS and NQO1 mRNA levels in HCC1937 cells[1].
WHN-11 perturbs protein homeostasis, including ubiquitination and proteasomal degradation in HCC1937 cells[1].
WHN-11 (0.1-40 μM, 1-16 h) activates apoptotic and autophagic signaling pathways in HCC1937 cells[1].
WHN-11 (1-50 μM) induces an indication of mitochondrial stress and dysfunction of HCC1937 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC1937 cells
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Concentration:0.1, 10 and 50 μM
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Incubation Time:1, 4 and 16 h
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Result:Induced both autophagy (as indicated by LC3B-I lipidation) and apoptosis (as indicated by caspase-3 cleavage) only after a prolonged exposure of 16 h.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Autophagy
- Apoptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- Macroautophagy Solutions
- Breast Cancer Modeling
Chemical Information
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Molecular Weight 539.59
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Formula C27H36F3N3O5
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SMILES
C[C@@H]1[C@@]2([H])[C@]34[C@](O[C@](OO3)(CC[C@@]4([H])[C@@H](CC2)C)C)([H])O[C@H]1N5CCN(CC5)C(NC6=CC=C(C=C6)C(F)(F)F)=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)