CPI-169

Catalog No.S7616

CPI-169 Chemical Structure

Molecular Weight(MW): 528.66

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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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.
Targets
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 M321fmZ2dmO2aX;uJIF{e2G7 Ml24O|IhcA>? MXjJcohq[mm2aX;uJI9nKEWcSEKgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gTFNMOjevZUOgcIV3\Wy|IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KEWOSWPBJI1mfGixZDygTWM2OD1yLkC4JO69VQ>? NHLIWZAzPjF6OUC3PC=>

... 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]

Protocol

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
  • Formulation: 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2O
  • 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 individually and in order:
10% DMSO+60% PEG 400+30% ddH2O
30mg/mL

* 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
Formula

C27H36N4O5S

CAS No. 1450655-76-1
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID