- GSK343
- 3-Deazaneplanocin A (DZNep) hydrochloride
- EI1
- EPZ005687
- 3-Deazaneplanocin,DZNep
| CPI-169EZH2 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
- View current batch:
- Purity = 99.47%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | a variety of cell lines |
Preparation method | The solubility of this compound in DMSO is >26.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | N/A |
Applications | In a variety of cell lines, CPI-169 inhibited the catalytic activity of PRC2 with IC50 value of < 1nm,="" decreased="" cellular="" levels="" of="" h3k27me3="" with="" ec50="" value="" of="" 70="" nm,="" and="" triggered="" cell="" cycle="" arrest="" and=""> |
| Animal experiment [1]: | |
Animal models | EZH2 mutant KARPAS-422 diffuse large B-cell lymphoma (DLBCL) xenograft |
Dosage form | 200 mpk twice daily (BID); administered subcutaneously |
Application | In EZH2 mutant KARPAS-422 diffuse large B-cell lymphoma (DLBCL) xenograft, CPI-169 is well tolerated in mice with no observed toxic effect or body weight loss. CPI-169 treatment led to tumor growth inhibition (TGI) in a dose-dependent way and reduced the pharmacodynamic marker H3K27me3. The highest dose (200 mpk BID) led to complete tumor regression. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Vidya Balasubramanian, Priya Iyer, Shilpi Arora, Patrick Troyer, Emmanuel Normant. Constellation Pharmaceuticals, Cambridge, MA. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivo and achieves complete regression in lymphoma xenograft models. | |
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| Cas No. | 1450655-76-1 | SDF | Download SDF |
| Chemical Name | (R,Z)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((2-hydroxy-4-methoxy-6-methylpyridin-3-yl)methyl)-2-methyl-1H-indole-3-carbimidic acid | ||
| Canonical SMILES | CCS(N1CCC([C@@](N2C(C)=C(/C(O)=N/CC(C(O)=N3)=C(OC)C=C3C)C4=CC=CC=C42)([H])C)CC1)(=O)=O | ||
| Formula | C27H36N4O5S | M.Wt | 528.66 |
| Solubility | ≥26.45mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | 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. | ||
CPI-169 is a novel, small molecule and potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of <1nm for="" polycomb="" repressive="" complex="" 2="" (prc2)="">
CPI-169 has been found to be a potent EZH2 inhibitor with an IC50 value of <1nm for="" polycomb="" repressive="" complex="" 2="" (prc2).="" in="" addition,="" cpi-169="" has="" been="" reported="" to="" reduce="" cellular="" levels="" of="" histone="" h3="" on="" lysine="" 27(h3k27)="" with="" an="" ec50="" value="" of="" 70nm.="" moreover,="" cpi-169="" has="" been="" exhibited="" to="" trigger="" cell="" cycle="" arrest="" and="" apoptosis="" in="" cells.="" apart="" from="" these,="" treatment="" the="" inhibitor="" at="" 200mpk="" twice="" daily,="" cpi-169="" has="" been="" noted="" to="" have="" a="" well="" tolerated="" in="" mice="" with="" no="" observed="" toxic="" effect="" or="" body="" weight="" loss="">
References:[1] Vidya Balasubramanian, Priya Iyer, Shilpi Arora, Patrick Troyer, Emmanuel Normant. Constellation Pharmaceuticals, Cambridge, MA. CPI-169, a novel and potent EZH2 inhibitor, synergizes with CHOP in vivo and achieves complete regression in lymphoma xenograft models
