Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: UNC-0638
  • Price: $450.0/100mg $850.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao
Related CAS#:
1255580-76-7 1255517-77-1

1255580-76-7

1255580-76-7 structure
1255580-76-7 structure
  • Name: UNC0638
  • Chemical Name: 2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
  • CAS Number: 1255580-76-7
  • Molecular Formula: C30H47N5O2
  • Molecular Weight: 509.727
  • Catalog: Signaling Pathways Autophagy Autophagy
  • Create Date: 2017-10-13 22:58:19
  • Modify Date: 2024-01-02 22:09:03
  • UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
Name 2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine
Synonyms cc-643
UNC 0638
2-Cyclohexyl-N-(1-isopropyl-4-piperidinyl)-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
UNII-26A103L2FO
2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
UNC-0638
UNC0638
2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine
Description UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
Related Catalog
Target

IC50: <15 nM (G9a), 19±1 nM (GLP)[1]
In Vitro UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.The Ki of UNC0638 is determined to be 3.0±0.05 nM (n=2). Consistent with this, the Morrison Ki for UNC0638 is 3.7±0.2 nM (n=3). The selectivity of UNC0638 over a wide range of epigenetic targets is evaluated. Notably, UNC0638 is inactive against other H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL and SMYD3), H3K79 (DOT1L) and H4K20 (SETD8) methyltransferases, as well as PRDM1, PRDM10 and PRDM12. In addition, UNC0638 is inactive against protein arginine methyltransferases PRMT1 and PRMT3, and HTATIP, a histone acetyltransferase. Of note, UNC0638 has weak but measurable activity against JMJD2E (IC50=4,500±1,100 nM), a Jumonji protein demethylase and DNA methyltransferase DNMT1 (IC50=107,000±6,000 nM). Nevertheless, the selectivity of UNC0638 for G9a and GLP over JMJD2E is >200-fold, and selectivity for G9a and GLP over DNMT1 is >5,000-fold[1]. UNC0638 is a type of small molecule that can specifically inhibit the enzyme activity of histone methyltransferase EHMT and reduce the H3K9 dimethylation (H3K9me2) levels in cells[2].
Kinase Assay The enzymatic reactions are conducted in duplicate at room temperature for 1 hour in a 50 μL mixture containing PKMT assay buffer, substrate coated plate, 10 M SAM, a HMT enzyme (EZH2 (800 ng/reaction), MLL (300 ng/reaction), PRMT1 (0.5 ng/reaction), SUV39H1 (75 ng/reaction) and UNC0638 (0-1.25 μM). After enzymatic reactions, 100 μL of first antibody is added to each well and the plate is incubated at room temperature for an additional 1 h. 100 μL of secondary antibody is added to each well and the plate is incubated at room temperature for an additional 30 min. 100 μL of developer reagents are added to wells and luminescence is measured using a BioTek SynergyTM 2 microplate reader. Enzyme activity assays are performed in duplicates at each concentration. The luminescence data are analyzed using the computer software, Graphpad Prism[1].
Cell Assay MDA-MB-231, PC3, HCT116 cells are cultured in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Cells are grown in the presence or absence of UNC0638 (10 nM, 100 nM, 1 μM, 10 μM, and 100 μM ) for stated amount of time. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1mg/mL of MTT and incubated for 1-2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazan is solubilized in acidified isopropanol and 1% Triton and absorbance measured at 570 nm, corrected for 650 nm background[1].
Animal Admin Mice[1] Standard DMPK studies in male Swiss albino mice (3 animals per data point) are conducted, following intravenous (IV, 1 mg/kg), oral (PO, 3 mg/kg), and intraperitoneal (IP, 2.5 mg/kg) administration of UNC0638.
References

[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.

[2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5.
Density 1.1±0.1 g/cm3
Boiling Point 563.9±50.0 °C at 760 mmHg
Melting Point 93-94 ºC
Molecular Formula C30H47N5O2
Molecular Weight 509.727
Flash Point 294.8±30.1 °C
Exact Mass 509.372986
PSA 62.75000
LogP 5.75
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.587
Storage condition -20℃
Water Solubility Practically insoluble (0.012 g/L) (25 ºC)
19748-66-4 structure

19748-66-4
1320288-42-3 structure

1320288-42-3

~%

1255580-76-7 structure

1255580-76-7
Literature: Liu, Feng; Barsyte-Lovejoy, Dalia; Allali-Hassani, Abdellah; He, Yunlong; Herold, J. Martin; Chen, Xin; Yates, Christopher M.; Frye, Stephen V.; Brown, Peter J.; Huang, Jing; Vedadi, Masoud; Arrowsmith, Cheryl H.; Jin, Jian Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6139 - 6150
385785-02-4 structure

385785-02-4

~%

1255580-76-7 structure

1255580-76-7
Literature: Liu, Feng; Barsyte-Lovejoy, Dalia; Allali-Hassani, Abdellah; He, Yunlong; Herold, J. Martin; Chen, Xin; Yates, Christopher M.; Frye, Stephen V.; Brown, Peter J.; Huang, Jing; Vedadi, Masoud; Arrowsmith, Cheryl H.; Jin, Jian Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6139 - 6150
385784-84-9 structure

385784-84-9

~%

1255580-76-7 structure

1255580-76-7
Literature: Liu, Feng; Barsyte-Lovejoy, Dalia; Allali-Hassani, Abdellah; He, Yunlong; Herold, J. Martin; Chen, Xin; Yates, Christopher M.; Frye, Stephen V.; Brown, Peter J.; Huang, Jing; Vedadi, Masoud; Arrowsmith, Cheryl H.; Jin, Jian Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6139 - 6150
1320288-38-7 structure

1320288-38-7

~%

1255580-76-7 structure

1255580-76-7
Literature: Liu, Feng; Barsyte-Lovejoy, Dalia; Allali-Hassani, Abdellah; He, Yunlong; Herold, J. Martin; Chen, Xin; Yates, Christopher M.; Frye, Stephen V.; Brown, Peter J.; Huang, Jing; Vedadi, Masoud; Arrowsmith, Cheryl H.; Jin, Jian Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6139 - 6150
4421-08-3 structure

4421-08-3

~%

1255580-76-7 structure

1255580-76-7
Literature: Liu, Feng; Barsyte-Lovejoy, Dalia; Allali-Hassani, Abdellah; He, Yunlong; Herold, J. Martin; Chen, Xin; Yates, Christopher M.; Frye, Stephen V.; Brown, Peter J.; Huang, Jing; Vedadi, Masoud; Arrowsmith, Cheryl H.; Jin, Jian Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6139 - 6150
52805-34-2 structure

52805-34-2

~%

1255580-76-7 structure

1255580-76-7
Literature: Liu, Feng; Barsyte-Lovejoy, Dalia; Allali-Hassani, Abdellah; He, Yunlong; Herold, J. Martin; Chen, Xin; Yates, Christopher M.; Frye, Stephen V.; Brown, Peter J.; Huang, Jing; Vedadi, Masoud; Arrowsmith, Cheryl H.; Jin, Jian Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6139 - 6150

Chemsrc provides CAS#:1255580-76-7 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 1255580-76-7 | Chemsrc address: https://www.chemsrc.com/en/baike/842933.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved