Cat. No.: HY-161303

ZNF207-IN-1

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ZNF207-IN-1 is an orally active and brain-penetrant ZNF207 inhibitor with a target K_D 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].

For research use only. We do not sell to patients.

Purity: 98.03%
CAS No.: 2923208-52-8
Formula: C₃₂H₃₂BrN₃O
Molecular Weight:554.52

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

ZNF207-IN-1 Chemical Structure

CAS No.: 2923208-52-8

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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 K_D 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.

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.

Chemical Information

CAS No. 2923208-52-8
Appearance Solid
Molecular Weight 554.52
Formula C₃₂H₃₂BrN₃O
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhang M, et al. Discovery of Novel N-(Anthracen-9-ylmethyl) Benzamide Derivatives as ZNF207 Inhibitors Promising in Treating Glioma. J Med Chem. 2024 Mar 14;67(5):3909-3934. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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ZNF207-IN-1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Cell Death Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

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ZNF207-IN-1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Biological Activity

Chemical Information

Purity & Documentation

References

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Help & FAQs

ZNF207-IN-1 Related Classifications

HY-161303 Related Classifications