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SML1037

Sigma-Aldrich

UNC0642

≥98% (HPLC)

同義詞:

2-(4,4-Difluoropiperidin-1-yl)-6-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-4-amine

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About This Item

經驗公式(希爾表示法):
C29H44F2N6O2
CAS號碼:
分子量::
546.70
MDL號碼:
分類程式碼代碼:
51111800
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 5 mg/mL, clear (warmed)

儲存溫度

2-8°C

SMILES 字串

FC(CC1)(F)CCN1C2=NC(NC3CCN(C(C)C)CC3)=C4C(C=C(OCCCN5CCCC5)C(OC)=C4)=N2

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)

InChI 密鑰

RNAMYOYQYRYFQY-UHFFFAOYSA-N

應用

UNC0642 has been used to treat human HeLa cells to inhibit the DNA ligase 1 (LIG1) /UHRF1 (ubiquitin-like with PHD and ring finger domains 1) interaction.

生化/生理作用

UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), which catalyze the mono and dimethylation of lysine 9 of histone 3 (H3K9), and other non-histone substrates such as p53 and WIZ. UNC0642 has an in vitro IC50 <15 nM with greater than 100-fold selectivity over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 has the same potency with improved PK properties relative to UNC0638, which should make it a more useful probe in an in vivo setting. For full characterization details, please visit the UNC0642 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

特點和優勢

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.
UNC0642 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.

其他說明

UNC0642 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the UNC0642 probe summary on the Chemical Probes Portal website.

相關產品

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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Tiffani D M Berkel et al.
The international journal of neuropsychopharmacology, 22(4), 292-302 (2018-12-28)
Tolerance to ethanol-induced anxiolysis promotes alcohol intake, thus contributing to alcohol use disorder development. Recent studies implicate histone deacetylase-mediated histone H3K9 deacetylation in regulating neuropeptide Y expression during rapid ethanol tolerance to the anxiolytic effects of ethanol. Furthermore, the histone
Yue-Peng Cao et al.
Acta pharmacologica Sinica, 40(8), 1076-1084 (2019-02-16)
Urinary bladder cancer (UBC) is characterized by frequent recurrence and metastasis despite the standard chemotherapy with gemcitabine and cisplatin combination. Histone modifiers are often dysregulated in cancer development, thus they can serve as an excellent drug targets for cancer therapy.
Patricia D B Tiburcio et al.
Translational oncology, 13(10), 100819-100819 (2020-07-06)
Malignant gliomas have disproportionally high morbidity and mortality. Heterozygous mutations in the isocitrate dehydrogenase 1 (IDH1) gene are most common in glioma, resulting in predominantly arginine to histidine substitution at codon 132. Because IDH1R132H requires a wild-type allele to produce
Methylation of DNA Ligase 1 by G9a/GLP Recruits UHRF1 to Replicating DNA and Regulates DNA Methylation.
Ferry L, et al.
Molecular Cell, 67(4), 550-565 (2017)
Chengfa Zhao et al.
Reproduction (Cambridge, England), 157(4), 359-369 (2019-02-08)
Somatic cell nuclear transfer in mammalian cloning suffers from a faulty epigenetic reprogramming, which is believed to cause developmental failures in cloned embryos. Regulating the epigenetic-modifying enzymes can rescue the chromatin of cloned embryos from aberrant epigenetic status, thereby potentially

文章

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

我們提供各種小分子研究工具,例如轉錄因子調節劑、染色質修飾酵素的抑制劑,以及用於基因調控研究中靶點鑑定和驗證的激效劑/拮抗劑;以下是這些研究工具的精選。

我們的科學家團隊在所有研究領域都有豐富的經驗,包括生命科學、材料科學、化學合成、色譜、分析等.

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