UNC0642 --- G9a/GLP HMTase Inhibitor


Catalog No. size PriceQuantity
M60185-2S 2 mg solid $129
M60185-10S 10mg solid $522

Description

UNC0642 is a novel highly potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC50 < 2.5 nM. It has selectivity > 1000-fold over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50~110 nM). It has improved PK properties relative to UNC0638 and displayed modest brain penetration in vivo.

Product information

CAS Number: 1481677-78-4

Molecular Weight: 546.70

Formula: C29H44F2N6O2

Chemical Name: 2-(4,4-difluoropiperidin-1-yl)-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine

Smiles: CC(C)N1CCC(CC1)NC1=NC(=NC2=CC(OCCCN3CCCC3)=C(C=C21)OC)N1CCC(F)(F)CC1

InChiKey: RNAMYOYQYRYFQY-UHFFFAOYSA-N

InChi: InChI=1S/C29H44F2N6O2/c1-21(2)36-14-7-22(8-15-36)32-27-23-19-25(38-3)26(39-18-6-13-35-11-4-5-12-35)20-24(23)33-28(34-27)37-16-9-29(30,31)10-17-37/h19-22H,4-18H2,1-3H3,(H,32,33,34)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

UNC0642 was used at 0.5 µM in vitro and cellular assays.

In Vivo:

UNC0642 was dosed to mice by intraperitoneal injection (IP) at 5 mg/kg once per day.

References:

  1. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. (2013) J Med Chem. 56(21):8931-42.

Products are for research use only. Not for human use.


Documents

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed