OICR-9429

Catalog No.S7833

For research use only.

OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.

OICR-9429 Chemical Structure

CAS No. 1801787-56-3

Selleck's OICR-9429 has been cited by 6 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.
Targets
Wdr5-MLL interaction [1] WDR5 [1]
93 nM(Kd)
In vitro

OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM)[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21(DE3)-V2R-pRARE2 NV;uVmU{TnWwY4Tpc44h[XO|YYm= M{fTeWJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gdI9tgSCKaYOteIFo\2WmIGfEVlUhMDFidH:gN|M1KHKnc3nkeYV{MSCneIDy[ZN{\WRiaX6gSZNkcGW{aXPobYEh[2:uaTDCUFIyMESHMzmtWlJTNXCUQWLFNkBk\WyuczDifUB{fXKoYXPlJJBt[XOvb36gdoV{d26jbnPlJIFv[Wy7c3nzMEBM\D1yLkCz{txO MoDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NUi3NFMoRjJ4OUW4O|A{RC:jPh?=
BL21(DE3)-V2R-pRARE2 M2LhbGZ2dmO2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJJBwdHliSHnzMZRi\2enZDDXSHI2KChzIITvJFM{PCC{ZYPp[JVmeyliaX70[ZJi[3Srb36ge4l1cCCPTFyxJIF{e2W|c3XkJIF{KGSrc4DsZYNmdWWwdDDv[kBndHWxcnXzZ4VqdiCrc3;0bIlw[3mjbnH0[UBt[WKnbHzl[EA6NUGuYT3GRW0heGWydHnk[UB{fWK|dILheIUh\nKxbTDXSHI2KGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIFLMNlEpTEV|KT3WNnIueFKDUlWyJINmdGy|IHL5JIZtfW:{ZYPj[Y4tKEt;MD6wOu69VQ>? MlPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NUi3NFMoRjJ4OUW4O|A{RC:jPh?=
Assay
Methods Test Index PMID
Western blot Wdr5 / MLL / RbBP5 26167872

Protocol (from reference)

Cell Research:[1]
  • Cell lines: Primary human AML cells
  • Concentrations: 5 μM
  • Incubation Time: 72 h
  • Method: 20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 555.59
Formula

C29H32F3N5O3

CAS No. 1801787-56-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C2=C(C=C(C=C2)C3=CC=CC(=C3)CN4CCOCC4)NC(=O)C5=CNC(=O)C=C5C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy OICR-9429|OICR-9429 ic50|OICR-9429 price|OICR-9429 cost|OICR-9429 solubility dmso|OICR-9429 purchase|OICR-9429 manufacturer|OICR-9429 research buy|OICR-9429 order|OICR-9429 mouse|OICR-9429 chemical structure|OICR-9429 mw|OICR-9429 molecular weight|OICR-9429 datasheet|OICR-9429 supplier|OICR-9429 in vitro|OICR-9429 cell line|OICR-9429 concentration|OICR-9429 nmr|OICR-9429 in vivo|OICR-9429 clinical trial|OICR-9429 inhibitor|OICR-9429 Epigenetics inhibitor