BIX 01294
Chemical Name: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride
Purity: ≥98%
Biological Activity
BIX 01294 is a GLP and G9a histone lysine methyltransferase inhibitor (IC50 values are 0.7 and 1.7 μM respectively) that displays no activity at other histone methyltransferases up to 37 μM. Modulates H3K9me2 levels in mammalian cells and potentiates induction of pluripotent stem cells from somatic cells in vitro. Also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3 (IC50 values are 40 - 112 μM). Restores metabolic and antiviral function in exhausted CD8+ T cells from patients with chronic HCV infection.For more information about how BIX 01294 trihydrochloride may be used, see our protocol: Converting Fibroblasts into Cardiomyocytes (9C Cocktail)
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of BIX-01294 is reviewed on the chemical probes website.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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IGF1R as a Key Target in High Risk, Metastatic Medulloblastoma
Matthew N Svalina
Sci Rep, 2016;6(0):27012. -
Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds.
Shi et al.
Cell Stem Cell., 2008;3:568 -
Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum.
Malmquist et al.
Proc.Natl.Acad.Sci.U.S.A., 2012;109:16708 -
BIX-01294 inhibits oncoproteins NSD1, NSD2, and NSD3.
Morishita et al.
Med.Chem.Res., 2017;26:2038 -
Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
Kubicek et al.
Mol.Cell, 2007;25:473 -
Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.
Chang et al.
Nat.Struct.Mol.Biol., 2009;16:312 -
Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection.
Barili et al.
Nat.Commun., 2020;11:604
Product Datasheets
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Citations for BIX 01294
The citations listed below are publications that use Tocris products. Selected citations for BIX 01294 include:
4 Citations: Showing 1 - 4
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Increased Efficacy of Histone Methyltransferase G9a Inhibitors Against MYCN-Amplified Neuroblastoma.
Authors: Bellamy Et al.
Front Oncol 2020;10
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Negative regulation of p53-induced senescence by N-WASP is crucial for DMBA/TPA-induced skin tumor formation.
Authors: Li Et al.
Cancer Res 2019;
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Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation.
Authors: Li Et al.
Nat Commun 2018;9:1420
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Activation of pluripotency genes in human fibroblast cells by a novel mRNA based approach.
Authors: Plews Et al.
Diabetes 2011;5:e14397
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