CPI-455 |
| Catalog No.GC10774 |
KDM5 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1628208-23-0
Sample solution is provided at 25 µL, 10mM.
IC50: 10 nM
CPI-455 is a KDM5 inhibitor.
The KDM5 family of histone demethylases catalyzes the demethylation of histone H3 on lysine 4 (H3K4) and is required for the survival of drug-tolerant persister cancer cells (DTPs).
In vitro: Previous study found that CPI-455 could potently inhibit the fulllength KDM5A in enzymatic assays with a half-maximal inhibitory concentration of 10 ± 1 nM. CPI-455 inhibited KDM5A, KDM5B and KDM5C to similar levels but showed significantly weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no detectable inhibition of KDM2B, KDM3B or KDM6A. Moreover, it was found that the CPI-455-mediated KDM5 inhibition led to a dose-dependent increase in global H3K4me3 in HeLa cells, and the removal of CPI-455 resulted in a rapid reversal of H3K4me3 increases in HeLa cells. Moreover, CPI-455 could delay the appearance of heavy H3K4me3, which was consistent with the role for KDM5 enzymes in H3K4me3 turnover, however, the turnover of H3K4me2 was only marginally altered. As expected, CPI-455 could affect the turnover of H3K4 monomethylation [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, CPI-455 is still in the preclinical development stage.
Reference:
[1] Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8.
Cell experiment: | MCF-7 is a luminal breast cancer cell line. MCF-7 is grown in MEM supplemented with 10% fetal bovine serum (FBS) and is incubated at 37°C with a 5% CO2 atmosphere. For each treatment condition, 2.5×105 MCF-7 cells are plated in T25 flask and allowed to rest overnight. The following day, the media is aspirated and replaced with media containing DAC at a final concentration of 62.5 nM. DAC media is aspirated and replaced every 24 hours for a total treatment time of 72 hours. Following DAC treatment, media is aspirated and replaced with media supplemented with 2% FBS containing KDM5 inhibitors (e.g., CPI-455) at a final concentration of 9.375 μM. Cells are harvested following 72 hours of KDM5 inhibitor treatment[1]. |
References: [1]. Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8. | |
| Cas No. | 1628208-23-0 | SDF | |
| Chemical Name | 6-isopropyl-7-oxo-5-phenyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile hydrochloride | ||
| Canonical SMILES | N#CC1=C(NC(C2=CC=CC=C2)=C(C(C)C)C3=O)N3N=C1.Cl | ||
| Formula | C16H15ClN4O | M.Wt | 314.77 |
| Solubility | ≥ 31.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1769 mL | 15.8846 mL | 31.7692 mL |
| 5 mM | 0.6354 mL | 3.1769 mL | 6.3538 mL |
| 10 mM | 0.3177 mL | 1.5885 mL | 3.1769 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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