LQZ-7
LQZ-7 is a survivin inhibitor and molecular glue degrader (Kd=0.24 μM). LQZ-7 binds to the dimerization interface of survivin, disrupting homodimerization and dissociating dimeric survivin into monomers, thereby accelerating its proteasome-dependent degradation. LQZ-7 does not affect the structurally similar dimeric proteins 14-3-3σ and 14-3-3δ, and can induce apoptosis, exhibiting cytotoxicity against cancer cells.
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- CAS 番号: 1044664-73-4
- 分子式: C24H19N7O4
- 分子量:469.45
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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
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
25 μM
|
Inhibitory concentration 50% against human PC-3 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
Inhibitory concentration 50% against human PC-3 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
|
26744521 |
| DU-145 | IC50 |
25 μM
|
Inhibitory concentration 50% against human DU145 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
Inhibitory concentration 50% against human DU145 cancer cells assessed as reduction in cell survival incubated for 3 days by MTT assay.
|
26744521 |
体外実験
LQZ-7 (30 min) dissociates existing dimeric survivin[1].
LQZ-7 (25 µM; 3 days) inhibits survival of PC-3 and DU145 cells with an IC50 of ~25 µM[1].
LQZ-7 (10 µM; 24 hours) induced survivin loss in PC-3 cells is reversed by proteasome inhibitors[1].
LQZ-7 induces proteasome-dependent degradation of survivin in cancer cells[2].
LQZ-7 (20 μM) binds to survivin, disrupts survivin dimerization, and accelerates proteasome-dependent degradation of survivin, exhibiting cytotoxicity against Du145 and PC3 cells with an IC50 of ~25 μM[3].
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:DU145 and PC-3
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Concentration:25 µM
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Incubation Time:3 days
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Result:Inhibited survival of human PC-3 and DU145 cells with an IC50 of ~25 µM.
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Cell Line:PC-3
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Concentration:10 µM
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Incubation Time:24 hours
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Result:Induced survivin loss that was reversed by co-treatment with a proteasome inhibitor, MG132 or bortezomib.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (male, 4-6 weeks old)[1]
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Dosage:25 mg/kg
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Administration:i.p.; every 3 days; 8 doses
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Result:Inhibited the growth of PC-3 xenograft tumors compared to the vehicle control.
Reduced final average tumor weight significantly compared to the control group.
Maintained constant body weight after multiple dosings.
Induced apoptosis, showing more apoptotic cells with condensed chromatin.
Dramatically reduced survivin levels as determined by Western blot and immunohistochemistry.
化学情報
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CAS 番号 1044664-73-4
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分子量 469.45
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分子式 C24H19N7O4
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SMILES
OC(C1=CC=CC(C2=CC=C(O2)/C=N/NC3=NC4=NON=C4N=C3NC5=C(C(C)=CC=C5)C)=C1)=O
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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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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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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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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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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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)