ZNF207-IN-1
Based on 1 Customer Validation
ZNF207-IN-1 is an orally active and brain-penetrant ZNF207 inhibitor with a target KD of 67 nM. ZNF207-IN-1 binds directly to ZNF207, downregulates stem-related genes and weakens glioma cell stemness. ZNF207-IN-1 hinders tumorigenesis and migration and promotes apoptosis. ZNF207-IN-1 can be used for the research of glioma[1].
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.03%
- CAS No.: 2923208-52-8
- 화학식: C32H32BrN3O
- 분자량:554.52
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
9.68 μM
Compound: C16
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| AGS | IC50 |
9.42 μM
Compound: C16
|
Antiproliferative activity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human AGS cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| H4 | IC50 |
0.72 μM
Compound: C16
|
Antiproliferative activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| H4 | IC50 |
0.74 μM
Compound: C16
|
Inhibition of sphere formation in human H4 cells incubated for 168 hrs by microscopic analysis
Inhibition of sphere formation in human H4 cells incubated for 168 hrs by microscopic analysis
|
[PMID: 38377560] |
| HeLa | IC50 |
8.13 μM
Compound: C16
|
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| Hs 683 | IC50 |
2.1 μM
Compound: C16
|
Inhibition of sphere formation in human Hs 683 cells incubated for 168 hrs by microscopic analysis
Inhibition of sphere formation in human Hs 683 cells incubated for 168 hrs by microscopic analysis
|
[PMID: 38377560] |
| Hs 683 | IC50 |
8.53 μM
Compound: C16
|
Antiproliferative activity against human Hs 683 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human Hs 683 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| LN-229 | IC50 |
1.23 μM
Compound: C16
|
Inhibition of sphere formation in human LN-229 cells incubated for 168 hrs by microscopic analysis
Inhibition of sphere formation in human LN-229 cells incubated for 168 hrs by microscopic analysis
|
[PMID: 38377560] |
| LN-229 | IC50 |
4.99 μM
Compound: C16
|
Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human LN-229 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| MKN-45 | IC50 |
3.84 μM
Compound: C16
|
Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| NCI-H460 | IC50 |
15.64 μM
Compound: C16
|
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| U-251 | IC50 |
0.87 μM
Compound: C16
|
Inhibition of sphere formation in human U-251MG cells incubated for 168 hrs by microscopic analysis
Inhibition of sphere formation in human U-251MG cells incubated for 168 hrs by microscopic analysis
|
[PMID: 38377560] |
| U-251 | IC50 |
13.09 μM
Compound: C16
|
Antiproliferative activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
| U-937 | IC50 |
13.97 μM
Compound: C16
|
Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 38377560] |
In Vitro
ZNF207-IN-1 (Compound C16) (19.5-625 nM) potently binds to purified ZNF207 protein with a KD of 67 nM[1].
ZNF207-IN-1 (30 μM; 3 h) directly binds to endogenous ZNF207 in H4 and U251MG glioma cells[1].
ZNF207-IN-1 potently inhibits the proliferation of H4, LN229, HS683, and U251MG glioma cells with IC50 values ranging from 0.72 to 13.09 μM[1].
ZNF207-IN-1 inhibits the proliferation of Hela, U-937, A549, H460, MKN45, and AGS non-glioma cancer cells with IC50 values ranging from 3.84 to 15.64 μM[1].
ZNF207-IN-1 (0.625-10 μM; 168 h) potently inhibits sphere formation (a marker of cancer stem cell activity) in H4, LN229, HS683, and U251MG glioma cells with IC50 values ranging from 0.74 to 2.10 μM[1].
ZNF207-IN-1 (1-8 μM; 10 days) dose-dependently reduces the sphere-initiating frequency of H4, LN229, HS683, and U251MG glioma cells, with up to a 166-fold reduction at 8 μM[1].
ZNF207-IN-1 (0.625-5 μM; 24 h) dose-dependently inhibits colony formation in H4, LN229, HS683, and U251MG glioma cells, with complete inhibition at 2.5 μM for LN229 and U251MG, and 5 μM for H4 and HS683[1].
ZNF207-IN-1 (0.625-2.5 μM; 24 h) dose-dependently induces apoptosis in U251MG and HS683 glioma cells[1].
ZNF207-IN-1 (2.5-10 μM; 24-48 h) dose-dependently inhibits the migration of LN229 glioma cells[1].
ZNF207-IN-1 (0.625-4 μM; 48 h) downregulates the expression of multiple stemness-related genes in LN229 and U251MG glioma cells, with a more pronounced effect in glioma spheres[1].
ZNF207-IN-1 (2-4 μM; 48 h) significantly reduces SOX2 protein expression in H4 and LN229 glioma cells at concentrations of 2 and 4 μM after 48 h[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:U251MG, HS683 glioma cell lines
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Concentration:0.625 μM; 1.25 μM; 2.5 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner; detected approximately 20% apoptotic cells in U251MG and HS683 cultures treated with 2.5 μM for 24 h.
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Cell Line:LN229 glioma cell line
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Concentration:2.5 μM; 5 μM; 10 μM
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Incubation Time:24 h; 48 h
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Result:Reduced wound closure in a dose-dependent manner.
At 5 μM, inhibited wound healing by 16.6% after 24 h and 28.4% after 48 h compared to DMSO controls.
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Cell Line:U251MG, LN229 glioma cell lines
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Concentration:0.625 μM; 1.25 μM; 2 μM; 4 μM
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Incubation Time:48 h
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Result:Decreased the RNA levels of EpCAM, OCT4, c-Myc, CD24, NANOG, SOX2, CD133, and BMI-1.
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Cell Line:H4, LN229 glioma cell lines
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Concentration:2 μM; 4 μM
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Incubation Time:48 h
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Result:Significantly reduced SOX2 protein expression in H4 and LN229 cells.
In Vivo
ZNF207-IN-1 (15-45 mg/kg; p.o.; daily) significantly reduces tumor load by 7.6-fold and prolongs overall survival in an orthotopic glioma xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6−8 weeks old, injected LN229 cells subcutaneously into the right flank of mice with Matrig to establish an orthotopic glioma xenograft model)[1]
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Dosage:15 mg/kg; 45 mg/kg
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Administration:p.o.; daily; 46 days
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Result:Achieved approximately 55% tumor growth inhibition at both 15 mg/kg and 45 mg/kg doses compared to vehicle group.
Reduced average tumor volume to 280 cm3 at 15 mg/kg and 200 cm3 at 45 mg/kg on day 49, compared to >700 cm3 in vehicle group.
Decreased the proportion of Ki-67-positive cancer cells in treated xenografts.
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Animal Model:BALB/c nude (male, 6−8 weeks old, injected LN229 cells subcutaneously into the right flank of mice with Matrig to establish an orthotopic glioma xenograft model)[1]
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Dosage:15 mg/kg; 45 mg/kg
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Administration:p.o.; daily
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Result:Reduced tumor load by 7.6-fold on day 25 at 45 mg/kg dose compared to vehicle group (P = 0.0047).
Prolonged overall survival significantly at 45 mg/kg dose compared to vehicle group (P = 0.0062), with no significant difference compared to Temozolomide-treated group.
Provided minimal survival benefit at 15 mg/kg dose.
Chemical Information
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CAS No. 2923208-52-8
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Appearance Solid
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분자량 554.52
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화학식 C32H32BrN3O
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Color Off-white to light yellow
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SMILES
N#CC1(CC2(C3=C(C1C4=C2C=CC=C4)C=CC=C3)Br)C(NCCC5CCN(CC5)CC6=CC=CC=C6)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocol
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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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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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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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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
순도&문서
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)