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 NameBIX 01294, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine hydrate trihydrochloride
CAS935693-62-2
CBNumberCB42095439
MFC28H38N6O2
MW490.64
MDL NumberMFCD11045283
MOL File935693-62-2.mol
MSDS FileSDS

Chemical Properties

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).
pka	9.34±0.70(Predicted)
form	Off-white solid
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
FDA UNII	2PZ9U8BQ9B

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

Product number	Packaging	Price	Product description	Buy
Sigma-Aldrich 382190	5mg	$259	Histone Lysine Methyltransferase Inhibitor	Buy
Tocris 3364	10	$212	BIX01294 ≥98%(HPLC)	Buy
Tocris 3364	50	$887	BIX01294 ≥98%(HPLC)	Buy
TRC B591595	500mg	$1200	BIX01294	Buy
Usbiological 044611	1mg	$277	BIX 01294	Buy

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

Preparation Products And Raw materials

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

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32957	60
Alchem Pharmtech,Inc.	8485655694	sales@alchempharmtech.com	United States	63687	58
career henan chemical co	+86-0371-86658258 +8613203830695	factory@coreychem.com	China	29811	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	32165	58
Dayang Chem (Hangzhou) Co.,Ltd.	571-88938639 +8617705817739	info@dycnchem.com	China	52849	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10473	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
Coresyn Pharmatech Co., Ltd.	+86-571-86626709 +86-18157142896	cbc@coresyn.com	China	9984	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3135	58
TargetMol Chemicals Inc.		support@targetmol.com	United States	38632	58

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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 Spectrum

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

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