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382192

HMTase Inhibitor IV, UNC0638

Name: HMTase Inhibitor IV, UNC0638
Brand: MM

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

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):

C₃₀H₄₇N₅O₂

CAS Number:

1255580-76-7

Molecular Weight:

509.73

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD22208587

Assay:

≥98% (HPLC)

Form:

powder

Storage condition:

OK to freeze, protect from light

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Properties

Quality Segment

100

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

Description

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 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.

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.

Legal Information

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

Disclaimer

Toxicity: Regulatory Review (Z)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c