ChemicalBook > CAS DataBase List > BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride

BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride

Product Name
BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride
CAS No.
935693-62-2
Chemical Name
BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride
Synonyms
CS-207;BIX 01294;BIX01294,BIX-01294;BIX 01294 (free base);EZSolution? BIX 01294;BIX-01294;BIX 01294; BIX01294;BIX 01294 hydrate trihydrochloride;Histone Lysine methyltransferase Inhibitor;Histone Lysine Methyltransferase Inhibitor - CAS 935693-62-2 - Calbiochem;N-(1-Benzyl-4-piperidinyl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-quinazolinamine
CBNumber
CB42095439
Molecular Formula
C28H38N6O2
Formula Weight
490.64
MOL File
935693-62-2.mol
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BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride Property

Boiling point:
654.6±65.0 °C(Predicted)
Density 
1.195±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
Soluble in DMSO (up to 50 mg/ml), or in Water (up to 50 mg/ml).
form 
Off-white solid
pka
9.34±0.70(Predicted)
color 
Off-white
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 3 months.
InChIKey
BZOWJAYUMMHCDW-UHFFFAOYSA-N
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
382190
Product name
Histone Lysine Methyltransferase Inhibitor
Packaging
5mg
Price
$259
Updated
2024/03/01
Tocris
Product number
3364
Product name
BIX01294
Purity
≥98%(HPLC)
Packaging
10
Price
$212
Updated
2021/12/16
Tocris
Product number
3364
Product name
BIX01294
Purity
≥98%(HPLC)
Packaging
50
Price
$887
Updated
2021/12/16
TRC
Product number
B591595
Product name
BIX01294
Packaging
500mg
Price
$1200
Updated
2021/12/16
Usbiological
Product number
044611
Product name
BIX 01294
Packaging
1mg
Price
$277
Updated
2021/12/16
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BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride Chemical Properties,Usage,Production

Description

BIX-01294 (935693-62-2) is a selective inhibitor of G9a histone methyltransferase (G9aHMTase; IC50 = 1.7 μM) as well as GLP HMTase (IC50 = 38 μM) leading to a decrease in H3K9me2(histone H3 lysine 9 methylation) in vitro.1 BIX-01294 facilitates the reactivation of pluripotency genes and induces passive demethylation, thus promoting reprogramming. BIX-01294, in combination with BAY K8644 (a calcium channel agonist), was found to improve reprogramming efficiencies of Oct4-Klf4-(OK)-infected neural progenitor cells.3

Uses

BIX 01294 is a euchromatic histone-lysine N-methyltransferase 2 (EHMT2) inhibitor, induces autophagy and apoptosis in human neuroblastoma cells, specifically human bladder cancer cells.

Definition

ChEBI: 6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine is a member of piperidines.

General Description

A cell-permeable diazepinyl-quinazolinamine, non-SAM (S-adenosylmethionine) analog-based HMTase (histone methyltransferase) inhibitor that selectively interferes with the G9a-catalyzed H3K9me2 (histone H3 Lys9 dimethylation) modification (IC50 = 1.7 μM) in a reversible manner. It inhibits the GLP-catalyzed H3K9me3 only at much higher concentrartions (IC50 = 38 μM) and exhibits little activity against H3 methylations catalyzed by other HMTases (PRMT1, SET7/9, ESET, SUV39H1). Shown to effectively synergize with Oct3/4 and Klf4 in inducing reprogramming of primary murine fetal NPCs (Neural Progenitor Cells) into iPS (induced Pluripotent Stem) cells without additional viral transduction of Sox2 and c-Myc.

Biological Activity

G9a-like protein and G9a histone lysine methyltransferase (HMTase) inhibitor (IC 50 values are 0.7 and 1.7 μ M respectively) that displays no activity at other HTMases up to 37 μ M. Modulates H3K9me2 levels in mammalian cells and potentiates induction of pluripotent stem cells from somatic cells in vitro .

target

G9a-like protein

References

1) Kubicek et al. (2007) Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase; Mol. Cell. 25 473 2) Huangfu et al. (2008) Induction of pluripotent stem cells by defined factors is greatly improved by small-molecule compounds; Nat. Biotechnol. 26 795 3) Shi et al., (2008) A combined chemical and genetic approach for the generation of induced pluripotent stem cells; Cell Stem Cell. 2 525

BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride Suppliers

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View Lastest Price from BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride manufacturers

Career Henan Chemical Co
Product
N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine 935693-62-2
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-30

935693-62-2, BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochlorideRelated Search:

Resveratrol Sodium 2-propylpentanoate Vorinostat N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

  • 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinaminetrihydrochloride
  • BIX 01294
  • BIX 01294 hydrate trihydrochloride
  • BIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride
  • BIX01294,BIX-01294
  • CS-207
  • Histone Lysine Methyltransferase Inhibitor - CAS 935693-62-2 - Calbiochem
  • 4-QuinazolinaMine, 2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6,7-diMethoxy-N-[1-(phenylMethyl)-4-piperidinyl]-
  • 2-(Hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6,7-diMethoxy-N-[1-(phenylMethyl)-4-piperidinyl]-4-quinazolinaMine hydrate trihydrochloride
  • BIX 01294 (free base)
  • 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine
  • Histone Lysine methyltransferase Inhibitor
  • BIX-01294;BIX 01294; BIX01294
  • N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine trih
  • N-(1-Benzyl-4-piperidinyl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-quinazolinamine
  • 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quina
  • EZSolution? BIX 01294
  • 2-(Hexahydro-4-Methyl-1H-1,4-Diazaze-1-Yl)-6,7-Dimethoxy-N-[1-(Phenylmethyl)-4-Piperidyl]-4-Quinazoline Amine
  • 935693-62-2
  • C28H41Cl3N6O2
  • C28H38N6O23HCl
  • C28H38N6O2
  • C28H43Cl3N6O3
  • Epigenetics
  • G9a-like protein and G9a histone lysine methyltransferase (HMTase) inhibitor.