IV-23
IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
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- CAS 番号: 2326007-49-0
- 分子式: C18H18BrNO4
- 分子量:392.24
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
6.82 μM
Compound: 9d
|
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 33965530] |
| A549 | IC50 |
6.82 μM
Compound: 9d
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
|
[PMID: 34022412] |
| ECa-109 cell line | IC50 |
2.24 μM
Compound: 9d
|
Antiproliferative activity against human Eca-109 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human Eca-109 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 33965530] |
| ECa-109 cell line | IC50 |
2.24 μM
Compound: 9d
|
Antiproliferative activity against human Eca-109 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human Eca-109 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
|
[PMID: 34022412] |
| KYSE-30 | IC50 |
1.61 μM
Compound: 9d
|
Antiproliferative activity against human KYSE-30 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human KYSE-30 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 33965530] |
| KYSE-30 | IC50 |
1.61 μM
Compound: 9d
|
Antiproliferative activity against human KYSE-30 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human KYSE-30 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
|
[PMID: 34022412] |
| KYSE-450 | IC50 |
1.49 μM
Compound: 9d
|
Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 33965530] |
| KYSE-450 | IC50 |
1.49 μM
Compound: 9d
|
Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
|
[PMID: 34022412] |
| KYSE-510 | IC50 |
2.08 μM
Compound: 9d
|
Antiproliferative activity against human KYSE-510 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human KYSE-510 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 33965530] |
| KYSE-510 | IC50 |
2.08 μM
Compound: 9d
|
Antiproliferative activity against human KYSE-510 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human KYSE-510 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
|
[PMID: 34022412] |
| MGC-803 | IC50 |
1.84 μM
Compound: 9d
|
Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 33965530] |
| MGC-803 | IC50 |
1.84 μM
Compound: 9d
|
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
|
[PMID: 34022412] |
体外実験
IV-23 (Compound 20) shows a strong inhibition against the ESCCs in a concentration depend manner, the IC50 values against the Kyse30 and Kyse450 cell lines were all less than 2 μM, presented in a dose-dependent manner. IV-23 triggeres caspases related apoptosis in ESCC cells[1].
IV-23 induces G2/M phase arrest[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 2326007-49-0
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分子量 392.24
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分子式 C18H18BrNO4
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SMILES
O=C(N1CCC2=C1C=CC(Br)=C2)C3=CC(OC)=C(OC)C(OC)=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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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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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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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
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Soft Agar Colony Formation Assay
Soft agar colony formation assay measures anchorage-independent growth, in which transformed or tumorigenic cells proliferate as colonies in a semisolid agar matrix while many non-transformed adherent cells fail to proliferate without attachment; classic studies showed that growth in semisolid medium correlates with tumorigenicity in nude mice, and later protocol papers describe the method as a stringent in vitro assay for malignant transformation. The readout is the number, size, morphology, or signal intensity of colonies formed within agar after incubation; published formats include manual colony counting after staining, 96-well or 384-well quantitative formats, DNA-binding dye detection, MTT/tetrazolium-based detection, digital image analysis, and PCR-based marker detection from soft agar cultures.
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Colony Formation (Clonogenic) Assay
The clonogenic (colony formation) assay measures the ability of a single cell to retain reproductive viability and form a macroscopic colony, typically defined as a cluster derived from one progenitor cell after a defined growth period. This assay is widely used to evaluate cell survival after exposure to ionizing radiation or cytotoxic treatments and is considered a standard method in radiation biology for generating dose-response relationships of reproductive cell death. Colony formation reflects long-term proliferative capacity rather than short-term metabolic activity, and survival is quantified by comparing treated versus untreated conditions based on colony number and derived survival fractions.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)