ChemicalBook CAS DataBase List 935693-62-2

935693-62-2

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	935693-62-2
Molecular Formula	C28H38N6O2
MDL Number	MFCD11045283
Molecular Weight	490.64
MOL File	935693-62-2.mol

Synonyms

CS-207 BIX 01294 BIX01294,BIX-01294 BIX 01294 (free base) 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 N-(1-Benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine trih 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quina 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine 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-quinazolinaminetrihydrochloride 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

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).
form	Off-white solid
pka	9.34±0.70(Predicted)
color	Off-white
Water Solubility	H2O: >20mg/mL
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
SMILES	N1=C2C(C=C(OC)C(OC)=C2)=C(NC2CCN(CC3=CC=CC=C3)CC2)N=C1N1CCCN(C)CC1

Safety Data

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

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

Spectrum Detail

Supplier

Dezhou LonWel Pharmaceutical Technology Co., Ltd.

Telephone 13761310616

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList20080/0_EN.htm

Shanghai Boyle Chemical Co., Ltd.

Telephone

Websitehttp://www.boylechem.com

3B Pharmachem (Wuhan) International Co.,Ltd.

Telephone821-50328103-801 18930552037

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList13285/0_EN.htm

Haoyuan Chemexpress Co., Ltd.

Telephone021-58950125

Websitehttp://gb.chemexpress.com.cn

Shanghai Aladdin Bio-Chem Technology Co.,LTD

Telephone400-6206333 13167063860

Websitehttp://www.aladdin-e.com/

Nanjing Dulai Biotechnology Co., Ltd.

Telephone025-846993838003-8003 18013301590

Websitehttp://www.njduly.com

EnliPharma Technology Co., Ltd

Telephone0551-66399836 18955197623

Websitehttp://www.enlipharma.com

Bide Pharmatech Ltd.

Telephone400-400-164-7117 18317119277

Websitehttp://www.bidepharm.com

ShangHai KenEn Chemical Technology Co., Ltd.

Telephone 13120367189

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16352/0_EN.htm

AdooQ Bioscience CHINA

Telephone025-58849295 18951903616;

Websitehttp://www.adooq.cn

Sigma-Aldrich

Telephone021-61415566 800-8193336

Websitehttps://www.sigmaaldrich.cn

Shanghaizehan biopharma technology co., Ltd.

Telephone021-61350663 13052117465

Websitehttp://www.zehanbiopharma.com

Guangzhou Zhiya Chemdrugs Co.,Ltd

Telephone 18122150900

Websitehttp://www.tiewill.com

SPIRO PHARMA

Telephone

Websitehttp://www.spiropharma.com.cn

Codow Chemical Co.,Ltd.

Telephone 18620099427

Websitehttp://www.howeipharm.com

ShangHai Siyan Biological Technology Co., Ltd.

Telephone021-50908862，442785678，326799392 18721037013

Websitehttp://www.siyanbio-tec.com

Guangzhou QiYun Biotechnology Co., Ltd.

Telephone020-61288194 61288195

Websitehttp://www.gzqiyun.com

Shanghai YuanYe Biotechnology Co., Ltd.

Telephone021-61312847; 18021002903

Websitehttp://www.shyuanye.com

1of4

Related Products

Send Inquriy