For research use only.

Catalog No.S7616

5 publications

CPI-169 Chemical Structure

CAS No. 1450655-76-1

CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

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Selleck's CPI-169 has been cited by 5 publications

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
EZH2 WT [1]
EZH2 Y641N [1]
EZH1 [1]
0.24 nM 0.51 nM 6.1 nM
In vitro

In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of <5 μM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hela cells NXvl[IVRTnWwY4Tpc44h[XO|YYm= MWe3NkBp M2LpN2lvcGmkaYTpc44hd2ZiRWrINkBqdiCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBJO0t{N33lN{Bt\X[nbIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliRVzJV2EhdWW2aH;kMEBKSzVyPUCuNFgh|ryP MmnrNlYyQDlyN{i=

... Click to View More Cell Line Experimental Data

In vivo In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects. [1]


Kinase Assay:[1]
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Biochemical Assays:

Compound potency is also assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, PRC2 containing either EZH1 (160 pM), wt EZH2 (40 pM), or Y641N mutant EZH2 (80 pM, both EZH2 prepared in-house) is pre-incubated with 3H-SAM (0.9 µM), 2 µM H3K27me3 activating peptide (H2N-RKQLATKAAR(Kme3)SAPATGGVKKP-amide) and compounds (as 10 point duplicate dose response titrations) for 120 min in a buffer consisting of 50 mM Tris (pH 8.5), 1 mM DTT, 0.07 mM Brij-35, 0.1% BSA, and 0.8% DMSO in a total volume of 12.5 µl in a black 384 well plate. Reaction is initiated with biotinylated H3 substrate peptides (H3K27me1 for wt EZH2, H3K27me2 for Y641N mutant EZH2; H2N-RKQLATKAAR(Kmen)SAPATGGVKKP-NTPEGBiot) as a 2 µM stock in 12.5 µL and allowed to react at room temperature for 5 h. Quenching is accomplished by addition of 20 µl of STOP solution (50 mM Tris (pH 8.5), 200 mM EDTA, 2 mM SAH). 35 µL of the quenched solution is transferred to Streptavidin Flashplates, incubated overnight, washed, and read in a TopCount Reader. For titrations all compound dilutions are in DMSO, final DMSO concentrations are 0.8% (v/v), and turnover is kept to less than < 5%. IC50s are calculated using non-linear least square four parameter fits (GraphPad 6.0).
Cell Research:[1]
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  • Cell lines: 25 NHL cell lines
  • Concentrations: ~10 μM
  • Incubation Time: 4 d
  • Method: Relative cell numbers are assessed by Cell Titer-Glo (CTG) luminescent cell viability assay using an Envision instrument. GraphPad Prism 6.0 is used for curve fitting, IC50/GI50 and Hill coefficient (H) calculations. The GI90 is calculated using the formula: EC90 = (90 /100-90)1/H * EC50.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Mice bearing KARPAS-422 subcutaneous xenografts
  • Dosages: 200 mg/kg, BID
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (189.15 mM)
Ethanol 100 mg/mL (189.15 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10% DMSO+60% PEG 400+30% ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 528.66


CAS No. 1450655-76-1
Storage powder
in solvent
Synonyms N/A
Smiles CCS(=O)(=O)N1CCC(CC1)C(C)N2C(=C(C3=CC=CC=C32)C(=O)NCC4=C(C=C(NC4=O)C)OC)C

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID