382190

Histone Lysine Methyltransferase Inhibitor

The Histone Lysine Methyltransferase Inhibitor, also referenced under CAS 935693-62-2, controls the biological activity of Histone Lysine Methyltransferase. This small molecule/inhibitor is primarily used for Cancer applications.

• 別名: Histone Lysine Methyltransferase Inhibitor, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-(1-(phenylmethyl)-4-piperidinyl)-4-quinazolinamine, BIX-01294, HMTase Inhibitor, EHMT2/G9a Inhibitor I, EHMT2/G9a Inhibitor I, HMTase Inhibitor, 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-(1-(phenylmethyl)-4-piperidinyl)-4-quinazolinamine, BIX-01294
• 実験式（ヒル表記法）: C₂₈H₃₈N₆O₂
• CAS番号: 935693-62-2
• 分子量: 490.64
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 10 mg/mL; ethanol: 10 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• InChI: 1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31)
• InChI Key: OSXFATOLZGZLSK-UHFFFAOYSA-N

詳細

詳細

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.

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 concentrations (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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

Shi, Y., et al. 2008. Cell Stem Cell2, 525.
Kubicek, S., et al. 2007. Mol. Cell25, 473.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable