2. Cell Cycle/DNA Damage Apoptosis
  3. Zinc Finger Protein Apoptosis
  4. ZNF207-IN-1

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].

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ZNF207-IN-1

ZNF207-IN-1 Chemical Structure

CAS No. : 2923208-52-8

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ZNF207-IN-1 Related Antibodies

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Description

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].

Cellular Effect
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.

ZNF207-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: U251MG, HS683 glioma cell lines
Concentration: 0.625 μM; 1.25 μM; 2.5 μM
Incubation Time: 24 h
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.

Cell Migration Assay [1]

Cell Line: LN229 glioma cell line
Concentration: 2.5 μM; 5 μM; 10 μM
Incubation Time: 24 h; 48 h
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.

Real Time qPCR[1]

Cell Line: U251MG, LN229 glioma cell lines
Concentration: 0.625 μM; 1.25 μM; 2 μM; 4 μM
Incubation Time: 48 h
Result: Decreased the RNA levels of EpCAM, OCT4, c-Myc, CD24, NANOG, SOX2, CD133, and BMI-1.

Western Blot Analysis[1]

Cell Line: H4, LN229 glioma cell lines
Concentration: 2 μM; 4 μM
Incubation Time: 48 h
Result: Significantly reduced SOX2 protein expression in H4 and LN229 cells.
In Vivo

ZNF207-IN-1 (Compound C16) (15-45 mg/kg; p.o.; daily; 46 days) achieves ~55% tumor growth inhibition in a subcutaneous glioma xenograft model[1].
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.

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]
Dosage: 15 mg/kg; 45 mg/kg
Administration: p.o.; daily; 46 days
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.
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]
Dosage: 15 mg/kg; 45 mg/kg
Administration: p.o.; daily
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.
Molecular Weight

554.52

Formula

C32H32BrN3O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1(CC2(C3=C(C1C4=C2C=CC=C4)C=CC=C3)Br)C(NCCC5CCN(CC5)CC6=CC=CC=C6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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ZNF207-IN-1 Related Classifications

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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.

Keywords:

ZNF207-IN-12923208-52-8Zinc Finger ProteinApoptosisglioma cellsHS683H4ZNF207migrationtumorigenesisLN229apoptosisgliomaU251MGInhibitorinhibitorinhibit

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