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
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
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.
N-Bromosuccinimide Price
- Product number
- 382190
- Product name
- Histone Lysine Methyltransferase Inhibitor
- Packaging
- 5mg
- Price
- $259
- Updated
- 2024/03/01
- Product number
- 3364
- Product name
- BIX01294
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $212
- Updated
- 2021/12/16
- Product number
- 3364
- Product name
- BIX01294
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $887
- Updated
- 2021/12/16
- Product number
- B591595
- Product name
- BIX01294
- Packaging
- 500mg
- Price
- $1200
- Updated
- 2021/12/16
- Product number
- 044611
- Product name
- BIX 01294
- Packaging
- 1mg
- Price
- $277
- Updated
- 2021/12/16
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
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
- Tel
- --
- Fax
- --
- chemist@dalton.com
- Country
- Canada
- ProdList
- 965
- Advantage
- 78
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
- 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