ZH25
ZH25 is an ATR kinase inhibitor with antiproliferative activity against ATM-deficient cancer cells. ZH25 induces DNA damage, reduces G2/M phase cell proportion, upregulates γH2AX, Cleaved-Caspase3, and Cleaved-PARP. ZH25 functions as an ATR kinase binding ligand for ATR-PROTAC degrader design. ZH25 can be used for the research of atm-deficient cancer.
For research use only. We do not sell to patients.
- CAS No.: 3037598-39-0
- Formula: C20H23N5O
- Molecular Weight:349.43
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
ZH25 (72 h) inhibits the proliferation of ATM-deficient LoVo cells with an IC50 of 32.8 μM, but has no activity against ATM-proficient HCT116 cells or normal NCM460 cells[1].
ZH25 (72 h) does not inhibit the proliferation of ATM-deficient NCI-H23 or GRANTA-519 cells, with IC50 values >50 μM for both cell lines[1].
ZH25 (10 μM; 72 h) induces a small increase in DNA damage in LoVo cells, and induces less DNA damage than the ATR degrader I-1 at lower concentrations[1].
ZH25 (10 μM; 48 h) induces apoptosis in LoVo cells, and induces less apoptosis than the ATR degrader I-1 at 5 μM[1].
ZH25 (10 μM; 48 h) reduces the proportion of LoVo cells in the G2/M phase[1].
ZH25 (6.25-25 μM; 24 h) slightly upregulates DNA damage and apoptosis markers in LoVo cells, with weaker activity than the ATR degrader I-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
CAS No. 3037598-39-0
-
Molecular Weight 349.43
-
Formula C20H23N5O
-
SMILES
C[C@@H]1COCCN1C2=NC(C3=CC=CC4=C3C=CN4)=NC5=C2CCNC5
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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
-
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.
-
Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
-
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)