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: ≥360 days 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.

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