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Chemical Structure| 2095432-28-1 Chemical Structure| 2095432-28-1

Structure of CPI-455 HCl
CAS No.: 2095432-28-1

Chemical Structure| 2095432-28-1

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CPI-455 HCl is an inhibitor of KDM5. It can elevate global levels of H3K4 trimethylation (H3K4me3) and decrease the number of DTPs in multiple cancer cell line models.

Synonyms: CPI-455 HCl

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Product Details of CPI-455 HCl

CAS No. :2095432-28-1
Formula : C16H15ClN4O
M.W : 314.77
SMILES Code : N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O.[H]Cl
Synonyms :
CPI-455 HCl
MDL No. :N/A
InChI Key :SNODPNXOTKXHHH-UHFFFAOYSA-N
Pubchem ID :129896721

Safety of CPI-455 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of CPI-455 HCl

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEI-OC1 cells 30 μM 24 hours To investigate the protective effect of CPI-455 on HEI-OC1 cells under cisplatin-induced stress, results showed that CPI-455 reduced ROS accumulation and improved mitochondrial membrane potential and oxidative phosphorylation. PMC9672031
NB4 cells 5 μM 4 days CPI-455 treatment significantly induced differentiation of NB4 cells, as evidenced by increased expression of CD11b and CD11c PMC8525237
NB4 cells 20 μM 4 days CPI-455 at 20 μM further increased the proportion of CD11b+ cells, indicating enhanced differentiation effect PMC8525237
Eca-109 cells 15 μM 48 hours CPI-455 significantly inhibited the proliferation of Eca-109 cells and induced apoptosis by regulating the expression of related genes. PMC8072195
RAW 264.7 cells 25 μM 48 hours To verify the effect of CPI-455 on the anti-inflammatory effect of EgCF by inhibiting KDM5B, the results showed that CPI-455 treatment restored the mRNA expression of IL-6 and TNF-α, indicating that CPI-455 attenuated the anti-inflammatory effect of EgCF PMC10492338
THP-1 cells 25 μM 48 hours To verify the effect of CPI-455 on the anti-inflammatory effect of EgCF by inhibiting KDM5B, the results showed that CPI-455 treatment significantly upregulated the mRNA expression of IL-6 and TNF-α, indicating that CPI-455 attenuated the anti-inflammatory effect of EgCF PMC10492338
LNCaP 25 µM, 50 µM 72 hours CPI-455 attenuated androgen-induced expression of the prototypical AR target gene, KLK3/PSA, and RNA sequencing revealed that CPI-455 significantly affected the androgen-regulated transcriptome. PMC10154691
LNCaP:C4-2 50 µM 72 hours CPI-455 impaired androgen induction of NKX3.1 and downregulated FOXA1 expression, whereas AR expression was unchanged. PMC10154691
FaDu cells >50 µM 72 hours Evaluate the effects of CPI-455 alone and in combination with olaparib and cisplatin on cell viability, showing that CPI-455 significantly affects cell viability at high concentrations. PMC11201379
SCC-040 cells >50 µM 72 hours Evaluate the effects of CPI-455 alone and in combination with olaparib and cisplatin on cell viability, showing that CPI-455 significantly affects cell viability at high concentrations. PMC11201379
hPDLSCs 10 nM To confirm the role of H3K4me3 PMC9046131

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice cisplatin-induced ototoxicity model intraperitoneal injection 0.5 mg/kg or 2 mg/kg once daily for 5 days To investigate the protective effect of CPI-455 against cisplatin-induced ototoxicity in vivo, results showed that CPI-455 significantly reduced hearing loss. PMC9672031

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.88mL

3.18mL

1.59mL

31.77mL

6.35mL

3.18mL

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