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CPI-169 racemate

Catalog No. T6809   CAS 1450655-76-1
Synonyms: CPI 169, CPI-169, CPI169

CPI-169 racemate (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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
CPI-169 racemate Chemical Structure
CPI-169 racemate, CAS 1450655-76-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 72.00
5 mg In stock $ 127.00
10 mg In stock $ 180.00
25 mg In stock $ 396.00
50 mg In stock $ 589.00
100 mg In stock $ 839.00
1 mL * 10 mM (in DMSO) In stock $ 148.00
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Purity: 99.14%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CPI-169 racemate (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&IC50 EZH2 Y641N:0.51 nM, EZH2 WT:0.24 nM, EZH1:6.1 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]
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 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 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 Animal Models: Mice bearing KARPAS-422 subcutaneous xenograftsFormulation: 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2ODosages: 200 mg/kg, BIDAdministration: s.c.
Synonyms CPI 169, CPI-169, CPI169
Molecular Weight 528.66
Formula C27H36N4O5S
CAS No. 1450655-76-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 93 mg/mL (175.9 mM)

DMSO: 93 mg/mL (175.9 mM)

TargetMolReferences and Literature

1. Bradley WD, et al. Chem Biol. 2014, 21(11), 1463-1475.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Anti-Aging Compound Library Bioactive Compound Library Inhibitor Library NO PAINS Compound Library Stem Cell Differentiation Compound Library Chromatin Modification Compound Library Reprogramming Compound Library

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Keywords

CPI-169 racemate 1450655-76-1 Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase CPI 169 CPI169 racemate CPI-169 CPI169 CPI 169 racemate inhibitor inhibit

 

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