1. Apoptosis Autophagy
  2. Apoptosis Autophagy
  3. 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).

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WHN-11

WHN-11 Chemical Structure

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Description

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)[1].

Cellular Effect
Cell Line 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.

Western Blot Analysis[1]

Cell Line: HCC1937 cells
Concentration: 0.1, 10 and 50 μM
Incubation Time: 1, 4 and 16 h
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.
Molecular Weight

539.59

Formula

C27H36F3N3O5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • 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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Product Name:
WHN-11
Cat. No.:
HY-175221
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