H1k
H1k, a Eudistomin Y derivative, is a lysosome-targeted antiproliferation agent. H1k increases the autophagy signal and downregulate the expression of cyclin-dependent kinase (CDK1) and cyclin B1. H1k can be used in research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 3039928-21-4
- Formula: C26H20N2O2
- Molecular Weight:392.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
14.8 μM
Compound: H1k
|
Cytotoxicity against human A549 cells assessed as cell inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell inhibition measured after 72 hrs by MTT assay
|
[PMID: 36774698] |
| HepG2 | IC50 |
9.6 μM
Compound: H1k
|
Cytotoxicity against human HepG2 cells assessed as cell inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as cell inhibition measured after 72 hrs by MTT assay
|
[PMID: 36774698] |
| LS180 | IC50 |
2.9 μM
Compound: H1k
|
Cytotoxicity against human LS180 cells assessed as cell inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human LS180 cells assessed as cell inhibition measured after 72 hrs by MTT assay
|
[PMID: 36774698] |
| MDA-MB-231 | IC50 |
20.5 μM
Compound: H1k
|
Cytotoxicity against human MDA-MB-231 cells assessed as cell inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell inhibition measured after 72 hrs by MTT assay
|
[PMID: 36774698] |
| SGC-7901 | IC50 |
12.1 μM
Compound: H1k
|
Cytotoxicity against human SGC-7901 cells assessed as cell inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human SGC-7901 cells assessed as cell inhibition measured after 72 hrs by MTT assay
|
[PMID: 36774698] |
In Vitro
H1k (72 h) has antiproliferation activity against LS-180, HepG-2, SGC-7901, A549 and MDA-MB-231 cells with IC50 values of 2.9, 9.6, 12.1, 14.8, and 20.5 μM, respectively[1].
H1k (0-50 μM; 24 h) triggers a distinct G2-M arrest in the MDA-MB-231 and SGC-7901 cells in a dose-dependent manner[1].
H1k (0-20 μM; 6 h; MDA-MB-231 cells) induces autophagy to exert its antiproliferative activity, and lysosomes are its functional targets[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:MDA-MB-231 and SGC-7901 cells
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Concentration:0, 5, 10, 20, 50 μM
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Incubation Time:24 hours
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Result:Arrested cell cycle at G2-M period in a dose-dependent manner.
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Cell Line:MDA-MB-231 and SGC-7901 cells
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Concentration:0, 5, 10, and 20 μM
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Incubation Time:6 hours
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Result:Increased the LC3B-I and LC3B-II levels at MDA-MB-231 cells in a dose-dependent manner.
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Cell Line:MDA-MB-231 and SGC-7901 cells
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Concentration:0, 5, 10, 20, 50 μM
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Incubation Time:6 hours
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Result:Inhibited antiproliferation of cancer cells and the downregulation of CDK1 and cyclin B1.
Chemical Information
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CAS No. 3039928-21-4
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Molecular Weight 392.45
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Formula C26H20N2O2
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SMILES
COC1=CC=C(C=C1)CN2C3=C(C4=C2C(C(C5=CC=CC=C5)=O)=NC=C4)C=CC=C3
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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.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)