BIX 01294

Catalog No.S8006

For research use only.

BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.

BIX 01294 Chemical Structure

CAS No. 1392399-03-9

Selleck's BIX 01294 has been cited by 28 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Targets
G9a [1]
(Cell-free assay)
2.7 μM
In vitro

BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. [1] BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells M{\JNWZ2dmO2aX;uJIF{e2G7 NGTSUXFKdmirYnn0bY9vKG:oIFXST|UheGixc4Doc5J6dGG2aX;uJIlvKHOxcnLpeI9tNXO2aX31cIF1\WRiaIXtZY4hUGWOYTDj[YxteyxiSVO1NF0xNjB3OTFOwG0> NYrKS3NHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OVY1ODdpPkKzOlU3PDB5PD;hQi=>
HeLa NVXHOo94TnWwY4Tpc44h[XO|YYm= M{K2U|QvPSCqcoO= MXnJcohq[mm2aX;uJI9nKEWkb3zheolzfXNiZ3z5Z49xem:2ZXnuM41ifHKreDDwdo91\WmwIG\QOFAh\W62comgbY4hcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC0MlUhcHK|IHLleIEudGGldHHtZZNmKHKncH;yeIVzKGG|c3H5MEBKSzVyIE2gNE46PjZizszNMi=> MlXlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4MkSzPFcoRjJ7NkK0N|g4RC:jPh?=
BL21 (DE3)-Gold NGTDOHFHfW6ldHnvckBie3OjeR?= M{C3TFIxKG2rboO= NYHrdY41UW6qaXLpeIlwdiCxZjDOMZRmem2rbnHsJIhmgGGqaYP0bYRqdmVvdHHn[4VlKGi3bXHuJGc6[SBqOUGzJJRwKDFzOUOgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKEKOMkGgLGRGOylvR3;s[EBk\WyuczD1d4lv\yCqaYP0c45mKEh|IDixJJRwKDF3IILld4llfWW|KTDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkAzOCCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCkeTDtZZN{KHOyZXP0do9u\XS{LDDJR|UxKD1iMT65JO69VS5? NESyNpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{eyNFU2Pyd-Mke3NlA2PTd:L3G+
HL60 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MmfrOFghcHK| MoC1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iMj6yJO69VS5? M{PpWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{mzPVQ5Lz5{N{O5N|k1QDxxYU6=
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HepG2 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MYC0PEBpenN? NGKxbVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gN{44KM7:TT6= NG\0cVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O5N|k1QCd-MkezPVM6PDh:L3G+
K562 NF71fY5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NIfKdlE1QCCqcoO= NI\XbFRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTCzMlkh|ryPLh?= MorYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|OUO5OFgoRjJ5M{mzPVQ5RC:jPh?=
MDA-MB-231 M1:xNWZ2dmO2aX;uJIF{e2G7 M{[zNlIh\GG7cx?= NEnP[YxKdmirYnn0bY9vKG:oIFe5ZUBqdiCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDIN2s6dWV{IHzleoVtKGGodHXyJFIh\GG7czDifUBqdW23bn;mcJVwemW|Y3XuZ4UhcW5vY3XscEB4\XO2ZYLuJIFv[Wy7c3nzMEBKSzVyIE2gOE42PjNizszNMi=> NInxVZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0NVM2Oyd-Mkm1OFE{PTN:L3G+
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BT-37 NVG0UHlpeUiWUzDhd5NigQ>? NICxb3FyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= M3;M[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NUD6UnVoeUiWUzDhd5NigQ>? M3PMPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NXn0NYtbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 MlrodWhVWyCjc4PhfS=> Mn\2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NYfvbVRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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wild type fibroblast cells NVvSc3JTeUiWUzDhd5NigQ>? MnnhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKGOxboTyc4whUGhid3ns[EB1gXCnIH\pZpJw[myjc4SgZ4VtdHN? NWjnZ2ZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Assay
Methods Test Index PMID
Western blot Cyclin D1 / CDK2 / CDK4 / CDK 6 / Cyclin E ; G9a / H3K9me2 ; Atg7 / Atg5 / Atg5-Atg12 / Atg3 / Atg12 / LC3B 25198515
Immunofluorescence Ran / H3K9me3 30565836
Growth inhibition assay Cell viability 26013382

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 98 mg/mL
(163.32 mM)
Water 98 mg/mL
(163.32 mM)
Ethanol '8 mg/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 600.02
Formula

C28H38N6O2.3HCl

CAS No. 1392399-03-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC.Cl.Cl.Cl

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

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