| CPI-455KDM5 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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- NMR (Nuclear Magnetic Resonance)
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Chemical structure
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| Cas No. | 1628208-23-0 | SDF | Download SDF |
| Synonyms | N/A | ||
| 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 |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
