U4885
UNC0638 hydrate
≥98% (HPLC)
Sinónimos:
2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy) quinazolin-4-amine
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Acerca de este artículo
Fórmula empírica (notación de Hill):
C30H47N5O2 · xH2O
Número CAS:
Peso molecular:
509.73 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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solid
InChI key
LLJGACAJGYXBTL-UHFFFAOYSA-N
SMILES string
O.COc1cc2c(NC3CCN(CC3)C(C)C)nc(nc2cc1OCCCN4CCCC4)C5CCCCC5
InChI
1S/C30H47N5O2.H2O/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);1H2
assay
≥98% (HPLC)
storage condition
protect from light
color
off-white
solubility
DMSO: >10 mg/mL
storage temp.
−20°C
Quality Level
General description
UNC0638 enhances the E-cadherin expression in gemcitabine-resistant cell line (PANC-1-R).
Application
UNC0638 has been used to block G9a (a lysine methyltransferase) function in C2C12 cells. UNC0638 has also been reported to decrease H3K9 dimethylation (H3K9me2) levels and inhibit cell death in hair cells.
UNC0638 hydrate has been used:
- in fractionation and isolation of human blood cells and cell nuclei
- in the analysis of human immunodeficiency virus (HIV) reactivation in latently infected cell line
- to determine the effect of G9a and its enzymatic activity on cisplatin resistance
Biochem/physiol Actions
Histone methyltransferase inhibitor (HMT); G9a/GLP selective methyltransferase chemical probe.
UNC0638 hydrate is a histone methyltransferase (HMT) inhibitor. UNC0638 shows selectivity for G9a (EHMT2) and GLP (EHMT1) methyltransferases, which catalyze the methylation of lysine 9 of histone 3 (H3K9) as well as other non-histone substrates. For full characterization details, please visit the UNC0638 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
Features and Benefits
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
UNC0638 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
Other Notes
UNC0638 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the UNC0638 probe summary on the Chemical Probes Portal website.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 2 Oral - Aquatic Chronic 4
Clase de almacenamiento
6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Genome-wide mapping of histone H3K9me2 in acute myeloid leukemia reveals large chromosomal domains associated with massive gene silencing and sites of genome instability
Salzberg AC, et al.
PLoS ONE, 12(3), e0173723-e0173723 (2017)
HIV-1 infection of microglial cells in a reconstituted humanized mouse model and identification of compounds that selectively reverse HIV latency
Llewellyn GN, et al.
Journal of Neurovirology, 1-12 (2017)
Histone methyltransferase G9a drives chemotherapy resistance by regulating the glutamate-cysteine ligase catalytic subunit in head and neck squamous cell carcinoma
Liu CW, et al.
Molecular Cancer Therapeutics, molcanther-molcan0567 (2017)
G9a orchestrates PCL3 and KDM7A to promote histone H3K27 methylation
Pan MR, et al.
Scientific Reports, 5, 18709-18709 (2015)
Tie-Gang Meng et al.
International journal of biological sciences, 18(11), 4513-4531 (2022-07-23)
During oocyte growth, various epigenetic modifications are gradually established, accompanied by accumulation of large amounts of mRNAs and proteins. However, little is known about the relationship between epigenetic modifications and meiotic progression. Here, by using Gdf9-Cre to achieve oocyte-specific ablation
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