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.
别名:
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
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关于此项目
经验公式（希尔记法）:
C30H47N5O2
化学文摘社编号:
分子量:
509.73
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
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 key
QOECJCJVIMVJGX-UHFFFAOYSA-N
General description
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 α1A, adrenergic α1B 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.
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.
Packaging
Packaged under inert gas
Other Notes
Vedadi, M., et al. 2011. Nat. Chem. Biol.7, 566.
Liu, F., et al. 2011. J. Med. Chem.54, 6139.
Liu, F., et al. 2011. J. Med. Chem.54, 6139.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable