Product Name :
UNC0642 — G9a/GLP HMTase Inhibitor
Description:
UNC0642 is a novel highly potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC50 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.
CAS:
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
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.
Additional information:
UNC0642 is a novel highly potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC50 1000-fold over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins.{{SS-208} medchemexpress|{SS-208} Epigenetics|{SS-208} Purity & Documentation|{SS-208} In Vitro|{SS-208} custom synthesis|{SS-208} Cancer} UNC0642 reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50~110 nM).{{Amcenestrant} medchemexpress|{Amcenestrant} Estrogen Receptor/ERR|{Amcenestrant} Purity & Documentation|{Amcenestrant} Formula|{Amcenestrant} supplier|{Amcenestrant} Cancer} It has improved PK properties relative to UNC0638 and displayed modest brain penetration in vivo.PMID:35345980 |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:|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||
