CPI-455 HCl

Catalog No.S8287

For research use only.

CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

CPI-455 HCl Chemical Structure

CAS No. 2095432-28-1

Selleck's CPI-455 HCl has been cited by 15 publications

Purity & Quality Control

Choose Selective Histone Demethylase Inhibitors

Biological Activity

Description CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
Targets
KDM5A [1]
(Cell-free assay)
10 nM
In vitro

CPI-455 has improved potency against KDM5A while demonstrating ~200-fold selectivity for KDM5A over KDM4C. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no measurable inhibition of KDM2B, KDM3B or KDM6A. CPI-455-mediated KDM5 inhibition results in a dose-dependent increase in global H3K4me3 in HeLa cells. CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 M3zVOGZ2dmO2aX;uJIF{e2G7 M1Wy[lEhcHJ? MUDJcohq[mm2aX;uJI9nKGi3bXHuJG4ufGW{bXnuZYwhTkyDRz;IbZMufGGpZ3XkJGtFVTWEIDiyJJRwKDd3MTDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPmPUBqdnOnY4SgZ4VtdHNidYPpcochUDNqMT2yNUlMPCiPZUOpMWdIUyiEaX;0bY4qNzJvT1egZZMhe3Wkc4TyZZRmKG2nYYP1doVlKGGodHXyJFEhcHJiYomgRYxxcGGuaYPhJIF{e2G7LDDJR|UxRTBwM{O3{txO NF7udFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEe0OVA6QCd-M{C3OFUxQTh:L3G+
Sf9 MX7GeY5kfGmxbjDhd5NigQ>? NYDPfoc3OSCqch?= M{ThWmlvcGmkaYTpc44hd2ZiaIXtZY4hSy22ZYLtbY5idCCITFHHMZRi\2enZDDLSG02SSBqMTD0c{AyODlyIILld4llfWW|KTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JIlve2WldDDj[YxteyC3c3nu[{BJOyhzLUKxLWs1ME2nMzmtS2dMMEKrb4TpckkwOi2RRzDhd{B{fWK|dILheIUhdWWjc4Xy[YQh[W[2ZYKgNUBpeiCkeTDBcJBp[Wyrc3GgZZN{[XluIFnDOVA:OC53MEdOwG0> M4ixSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{S1NFk5Lz5|MEe0OVA6QDxxYU6=
Sf9 NUHwOIZWTnWwY4Tpc44h[XO|YYm= Mkn0NUBpeg>? MXjJcohq[mm2aX;uJI9nKG[3bHytcIVv\3SqIHj1cYFvKE5vdHXycYlv[WxiRlzBS{9JcXNvdHHn[4VlKEuGTUXDJEgzKHSxIEG1OlAhemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIFizLFEuOjFrS{SoUYU{MS2JR1uoRolwfGmwKT:yMW9IKGG|IIP1ZpN1emG2ZTDt[YF{fXKnZDDh[pRmeiBzIHjyJIJ6KEGucHjhcIl{[SCjc4PhfUwhUUN3ME2zMlAy|ryP NY\aR|dDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C3OFUxQThpPkOwO|Q2ODl6PD;hQi=>
PC9 MkXySpVv[3Srb36gZZN{[Xl? Mmj0OEBl[Xm| MlLJTY5pcWKrdHnvckBw\iCNRF21RUBqdiCqdX3hckBRSzliY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gTFNMPG2nMzDs[ZZmdHNicILlbY5kfWKjdHXkJIZweiB2IHThfZMhdWWjc4Xy[YQhfXBidH:gNlQhcHK|IHL5JGVNUVODLDDFR|UxRTVwMt88US=> NVTGUVZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0O|Y1OjRpPkK3OFc3PDJ2PD;hQi=>
Sf9 NHzFflBHfW6ldHnvckBie3OjeR?= NH;YR4cyKGi{ MVLJcohq[mm2aX;uJI9nKGi3bXHuJGMufGW{bXnuZYwhTkyDRz30ZYdo\WRiS1TNOmIhMDFyNEOgeI8h\W6mIILld4llfWW|KTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JIlve2WldDDj[YxteyC3c3nu[{BJOyh{MT20OEkuUzJ5KF3lN{kuT0tqQnnveIlvMS9{LV;HJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkAyKGi{IHL5JGFteGijbHnzZUBie3OjeTygTWM2OD1zND6z{txO M4LpfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{S1NFk5Lz5|MEe0OVA6QDxxYU6=
MDA-MB-231 NVriT3FqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEXvXnI2OCC3TR?= M4fEPFczKGi{cx?= M1XkS2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhPTBidV2gZYZ1\XJiN{KgbJJ{KGK7IFHsZY1ieiCkbIXlJJN1[WmwaX7nJIJie2WmIH\seY9z\XOlZX7j[UBie3OjeR?= M33CcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{S1NFk5Lz5|MEe0OVA6QDxxYU6=

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: melanoma (M14), breast cancer (SKBR3) and NSCLC (PC9) cell lines
  • Concentrations: 0-25 μM
  • Incubation Time: 14-20 days
  • Method:

    All cell lines were treated with DMSO, CPI-4203 or CPI-455 for 5 d with two changes of medium and drug. Thereafter, the cells (PC9, Colo205, Hs888, M14, SKBR3 and EVSA-T) were plated at 2×105 cells in six-well plates in triplicate and treated for an additional 9-15 d, depending on the cell line model. The Incucyte HD imaging system was used to monitor numbers of drug-tolerant cells after cells were stained with Nuclear-ID Red stain.

Solubility (25°C)

In vitro

DMSO 10 mg/mL
(31.76 mM)
Water Insoluble
Ethanol ''2 mg/mL

Chemical Information

Molecular Weight 314.77
Formula

C16H15ClN4O

CAS No. 2095432-28-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3.Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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.

Handling Instructions

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