二氯苯并咪唑呋喃型核糖苷

二氯苯并咪唑呋喃型核糖苷用途

5,6-二氯苯并咪唑核糖是一种核苷类似物,可抑制几种羧基末端结构域(CTD)激酶,包括酪蛋白激酶II和CDKs[1][2][3][4]。5,6-二氯苯并咪唑核苷可触发人类结肠腺癌细胞的p53依赖性凋亡,而不会诱导健康细胞的遗传毒性应激[5]。

点击显示

二氯苯并咪唑呋喃型核糖苷名称

[ CAS 号 ]:
53-85-0

[ 中文名 ]:
5,6-二氯-1-β-D-呋喃核糖基苯并咪唑

[ 英文名 ]:
5,6-Dichlorobenzimidazole riboside

[中文别名 ]:

[英文别名 ]:

Benzimidazole, 5,6-dichloro-1-β-D-ribofuranosyl-
5,6-Dichloro-1-(β-D-ribofuranosyl)benzimidazole
DRB
5,6-Dichlorobenzimidazole riboside
5,6-Dichloro-1-β-D-ribofuranosylbenzimidazole
MFCD00036785
5,6-Dichlorobenzimidazole 1-β-D-Ribofuranoside

二氯苯并咪唑呋喃型核糖苷生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> CDK

[参考文献]

[1]. Zandomeni RO. Kinetics of inhibition by 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole on calf thymus casein kinase II. Biochem J. 1989 Sep 1;262(2):469-73.

[2]. Yankulov K, et al. The transcriptional elongation inhibitor 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole inhibits transcription factor IIH-associated protein kinase. J Biol Chem. 1995 Oct 13;270(41):23922-5.

[3]. Rickert P, et al. Cyclin C/CDK8 and cyclin H/CDK7/p36 are biochemically distinct CTD kinases. Oncogene. 1999 Jan 28;18(4):1093-102.

[4]. Schang LM. Cyclin-dependent kinases as cellular targets for antiviral drugs. J Antimicrob Chemother. 2002 Dec;50(6):779-92.

[5]. te Poele RH, et al. RNA synthesis block by 5, 6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) triggers p53-dependent apoptosis in human colon carcinoma cells. Oncogene. 1999 Oct 14;18(42):5765-72.

二氯苯并咪唑呋喃型核糖苷物理化学性质

[ 密度 ]:
1.8±0.1 g/cm3

[ 沸点 ]:
606.2±65.0 °C at 760 mmHg

[ 熔点 ]:
222-224ºC

[ 分子式 ]:
C₁₂H₁₂Cl₂N₂O₄

[ 分子量 ]:
319.141

[ 闪点 ]:
320.4±34.3 °C

[ 精确质量 ]:
318.017426

[ PSA ]:
87.74000

[ LogP ]:
2.05

[ 外观性状 ]:
白色至灰白色结晶固体

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.750

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
Soluble in DMSO to 75mMSoluble in dimethyl sulfoxide, hot ethanol, dimethyl formamide, (1:2) dimethyl formamide:Phosphate buffer saline, water, methanol and pyridine. Slightly soluble in aqueous buffers.

二氯苯并咪唑呋喃型核糖苷MSDS

详细MSDS(安全技术说明书)

二氯苯并咪唑呋喃型核糖苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DD7310000

CHEMICAL NAME :: Benzimidazole, 5,6-dichloro-1-beta-D-ribofuranosyl-

CAS REGISTRY NUMBER :: 53-85-0

BEILSTEIN REFERENCE NO. :: 0039123

LAST UPDATED :: 199806

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C12-H12-Cl2-N2-O4

MOLECULAR WEIGHT :: 319.16

WISWESSER LINE NOTATION :: T56 BN DNJ GG HG B- BT5OTJ CQ DQ E1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Human HeLa cell

DOSE/DURATION :: 40 umol/L

REFERENCE :: PNASA6 Proceedings of the National Academy of Sciences of the United States of America. (National Academy of Sciences, Printing & Pub. Office, 2101 Constitution Ave., Washington, DC 20418) V.1- 1915- Volume(issue)/page/year: 79,2569,1982

点击显示

二氯苯并咪唑呋喃型核糖苷安全信息

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
DD7310000

[ 海关编码 ]:
29349990

二氯苯并咪唑呋喃型核糖苷上下游产品

二氯苯并咪唑呋喃型核糖苷上游产品

二氯苯并咪唑呋喃型核糖苷下游产品

二氯苯并咪唑呋喃型核糖苷文献

Direct regulation of gonadotrophin-releasing hormone (GnRH) transcription by RF-amide-related peptide-3 and kisspeptin in a novel GnRH-secreting cell line, mHypoA-GnRH/GFP.

J. Neuroendocrinol. 26(12) , 888-97, (2014)

RF-amide-related peptide-3 [RFRP-3; also often referred to as the mammalian orthologue of the avian gonadotrophin-inhibitory hormone (GnIH)] and kisspeptin have emerged as potent modulators of neuroen...

GSK-3β Phosphorylation of Cytoplasmic Dynein Reduces Ndel1 Binding to Intermediate Chains and Alters Dynein Motility.

Traffic 16 , 941-61, (2015)

Glycogen synthase kinase 3 (GSK-3) has been linked to regulation of kinesin-dependent axonal transport in squid and flies, and to indirect regulation of cytoplasmic dynein. We have now found evidence ...

Upregulation of CYP1B1 expression by inflammatory cytokines is mediated by the p38 MAP kinase signal transduction pathway.

Carcinogenesis 35(11) , 2534-43, (2014)

Cytochrome P450 1B1 (CYP1B1) is an enzyme that has a unique tumor-specific pattern of expression and is capable of bioactivating a wide range of carcinogenic compounds. We have reported previously tha...

更多文献