SML3071
RG3039
≥98% (HPLC)
别名:
5-[[1-(2,6-Dichlorobenzyl)piperidin-4-yl]methoxy]quinazoline-2,4-diamine, 5-[[1-[(2,6-Dichlorophenyl)methyl]-4-piperidinyl]methoxy]-2,4-quinazolinediamine, D157495, PF 06687859, PF-06687859, PF06687859, RG 3039, RG-3039
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关于此项目
经验公式（希尔记法）:
C21H23Cl2N5O
化学文摘社编号:
分子量:
432.35
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
RG3039, ≥98% (HPLC)
InChI
1S/C21H23Cl2N5O/c22-15-3-1-4-16(23)14(15)11-28-9-7-13(8-10-28)12-29-18-6-2-5-17-19(18)20(24)27-21(25)26-17/h1-6,13H,7-12H2,(H4,24,25,26,27)
SMILES string
NC1=NC(N)=C2C(OCC3CCN(CC3)CC4=C(C=CC=C4Cl)Cl)=CC=CC2=N1
InChI key
MNLHFGXIUJNDAF-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Brain-penetrant, potent mRNA-decapping enzyme DcpS (m7GpppX diphosphatase) inhibitor within in vivo efficacy in a murine spinal muscular atrophy (SMA) model.
RG3039 is a brain-penetrant and potent inhibitor against the scavenger mRNA-decapping enzyme DcpS (m7GpppX diphosphatase) in vitro (mouse DcpS IC50 = 3.4 nM) and in mice in vivo (∼90% & ∼80% inhibition of brain DcpS, respectively, 2 h & 72 h post last 3 mg/kg daily ip. from P1 to P10). In a murine severe spinal muscular atrophy (SMA) model, RG3039 (10-20 mg/kg/d ip. from P1 till death) increases SMAΔ7 mice survival (by 26%) and motor function with a ∼50% increase of VGLUT1 synapses number on L3-L5 motor neurons (33.7/WT mice at P13 vs. 17.2/SMA mice without 26.1/SMA mice with RG3039 treatment).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Rocky G Gogliotti et al.
Human molecular genetics, 22(20), 4084-4101 (2013-06-06)
Spinal muscular atrophy (SMA) is caused by insufficient levels of the survival motor neuron (SMN) protein due to the functional loss of the SMN1 gene and the inability of its paralog, SMN2, to fully compensate due to reduced exon 7
Takuji Yamauchi et al.
Cancer cell, 33(3), 386-400 (2018-02-27)
To identify novel targets for acute myeloid leukemia (AML) therapy, we performed genome-wide CRISPR-Cas9 screening using AML cell lines, followed by a second screen in vivo. Here, we show that the mRNA decapping enzyme scavenger (DCPS) gene is essential for AML
Alyssa N Calder et al.
Journal of medicinal chemistry, 59(22), 10067-10083 (2016-08-05)
Spinal muscular atrophy (SMA) is an autosomal recessive neurodegenerative disease resulting from pathologically low levels of survival motor neuron (SMN) protein. The majority of mRNA from the SMN2 allele undergoes alternative splicing and excludes critical codons, causing an SMN protein
Blazej A Wojtczak et al.
Journal of the American Chemical Society, 140(18), 5987-5999 (2018-04-21)
The 5' cap consists of 7-methylguanosine (m7G) linked by a 5'-5'-triphosphate bridge to messenger RNA (mRNA) and acts as the master regulator of mRNA turnover and translation initiation in eukaryotes. Cap analogues that influence mRNA translation and turnover (either as
James P Van Meerbeke et al.
Human molecular genetics, 22(20), 4074-4083 (2013-06-04)
Spinal muscular atrophy (SMA) is caused by mutations of the survival motor neuron 1 (SMN1) gene, retention of the survival motor neuron 2 (SMN2) gene and insufficient expression of full-length survival motor neuron (SMN) protein. Quinazolines increase SMN2 promoter activity
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