382192

HMTase Inhibitor IV, UNC0638

The HMTase Inhibitor IV, UNC0638 controls the biological activity of HMTase. This small molecule/inhibitor is primarily used for Cancer applications.

• 同義詞: HMTase Inhibitor IV, UNC0638, DNA Methyltransferase Inhibitor III, DNA MTase Inhibitor III, EHMT1/GLP Inhibitor II, EHMT2/G9a Inhibitor IV, 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
• 經驗公式（希爾表示法）: C₃₀H₄₇N₅O₂
• CAS號碼: 1255580-76-7
• 分子量：: 509.73
• MDL號碼: MFCD22208587
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 10 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C
• SMILES 字串: CC(C)N(CC1)CCC1NC2=NC(C3CCCCC3)=NC4=C2C=C(C(OCCCN5CCCC5)=C4)OC
• InChI: 1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33)
• InChI 密鑰: QOECJCJVIMVJGX-UHFFFAOYSA-N

描述

一般說明

A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC₅₀ = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC₅₀ = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC₅₀ >10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC₅₀ = 81 nM; EC₅₀ = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α_1A, adrenergic α_1B and muscarinic _M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.

A cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC₅₀ = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC₅₀ = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC₅₀ >10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC₅₀ = 81 nM; EC₅₀ = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α_1A, adrenergic α_1B and muscarinic _M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.




This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the UNC0638 probe summary on the SGC website.

包裝

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

其他說明

Vedadi, M., et al. 2011. Nat. Chem. Biol.7, 566.

Liu, F., et al. 2011. J. Med. Chem.54, 6139.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 2
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable