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Merck
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文件

SML1697

Sigma-Aldrich

OGG1抑制剂O8

≥98% (HPLC)

同義詞:

3,4-二氯-苯并[b]噻吩-2-羧酸酰肼

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About This Item

經驗公式(希爾表示法):
C9H6Cl2N2OS
CAS號碼:
分子量::
261.13
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 5 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

ClC1=C(C(NN)=O)SC2=CC=CC(Cl)=C21

InChI

1S/C9H6Cl2N2OS/c10-4-2-1-3-5-6(4)7(11)8(15-5)9(14)13-12/h1-3H,12H2,(H,13,14)

InChI 密鑰

HSSHUDKWJRJKPV-UHFFFAOYSA-N

一般說明

抑制 8-氧代鸟嘌呤 DNA 糖基化酶-1(OGG1),可用于治疗某些类型的癌症的单一疗法或联合疗法。

生化/生理作用

OGG1 抑制剂 O8 是 8-氧鸟嘌呤 DNA 糖基化酶 1(OGG1)的有效抑制剂,该酶是 DNA 碱基切除修复(BER)途径的一部分,正在成为癌症治疗的药物靶标。 OGG1 抑制剂 O8 的 IC50 值为 220 nM,相对于其他几种 DNA 修复糖基化酶,其对 OGG1 的选择性为 >100 倍。 O8 在 OGG1 催化过程中通过抑制席夫碱的形成发挥作用。它不能阻止 OGG1 与包含 7,8-二氢-8-氧鸟嘌呤(8-氧代-瓜氨酸)的底物的 DNA 结合。

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

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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Mingxin Chang et al.
Frontiers in pharmacology, 11, 610205-610205 (2021-02-02)
Background: Oncogenic transformation is associated with elevated oxidative stress that promotes tumor progression but also renders cancer cells vulnerable to further oxidative insult. Agents that stimulate ROS generation or suppress antioxidant systems can drive oxidative pressure to toxic levels selectively
Nathan Donley et al.
ACS chemical biology, 10(10), 2334-2343 (2015-07-29)
The DNA base excision repair (BER) pathway, which utilizes DNA glycosylases to initiate repair of specific DNA lesions, is the major pathway for the repair of DNA damage induced by oxidation, alkylation, and deamination. Early results from clinical trials suggest
Yaoyao Xue et al.
Frontiers in immunology, 14, 1161160-1161160 (2023-08-21)
Interferons (IFNs) are secreted cytokines with the ability to activate expression of IFN stimulated genes that increase resistance of cells to virus infections. Activated transcription factors in conjunction with chromatin remodelers induce epigenetic changes that reprogram IFN responses. Unexpectedly, 8-oxoguanine
Xu Zheng et al.
Journal of innate immunity, 1-22 (2022-05-06)
The primary cause of morbidity and mortality from infection with respiratory syncytial virus (RSV) is the excessive innate immune response(s) (IIR) in which reactive oxygen species (ROS) play key role(s). However, the mechanisms for these processes are not fully understood.
Wenjing Hao et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 34(6), 7427-7441 (2020-05-08)
8-Oxoguanine DNA glycosylase1 (OGG1)-initiated base excision repair (BER) is the primary pathway to remove the pre-mutagenic 8-oxo-7,8-dihydroguanine (8-oxoG) from DNA. Recent studies documented 8-oxoG serves as an epigenetic-like mark and OGG1 modulates gene expression in oxidatively stressed cells. For this

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