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普卡酶素

DNA和RNA聚合酶抑制剂。DNA结合转录抑制剂。
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货号 (SKU) 包装规格 是否现货 价格 数量
P113149-1mg
1mg 现货 Stock Image
P113149-5mg
5mg 现货 Stock Image
P113149-25mg
25mg 现货 Stock Image

基本描述

别名 光辉酶素,金霉酸 | 普卡霉素 | 光辉霉素
英文别名 Mithramycin A | Aurlelic acid | DB06810 | PA-144 | MITHRAMYCINA | MITHRAMYCIN | BDBM50547623 | Plicamycin [USAN:USP:INN:BAN] | PLICAMYCIN [USAN] | D00468 | Antibiotic LA 7017 | Mithramycinum | Mitramycine | plicamycin | Aureolic acid | CCRIS 5629 | NJWSNN
规格或纯度 Moligand™, ≥95%
英文名称 Plicamycin
生化机理 抗癌抗生素。抑制转录和蛋白质合成。与原生染色质中的 DNA 结合。DNA 和 RNA 聚合酶抑制剂,DNA 结合转录抑制剂(Sp1 和 Sp3)。具有抗肿瘤活性。
储存温度 -20°C储存,充氩
运输条件 超低温冰袋运输
备注 如果有可能,您尽量在使用的当天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Mithramycin A is an antibiotic DNA/RNA polymerase and DNA binding transcriptional inhibitor observed to facilitate TNF-α and Fas-ligand induced apoptosis. As a DNA binding transcriptional inhibitor, mithramycin A binds to GC rich sequences located in the minor groove of DNA and is noted to be reversible and Mg2+ dependent. Additionally reported to a block transcriptional activation of the SV40 promoter via competitive binding against Sp1 transcription factor to GC rich areas in the early promoter. Mithramycin A is noted to supress TNF-α induced expression of fractalkine (CX3CL1) mRNA in a dose-dependent manner and to act as an effective differentiation agent of HL60 promyelocytic leukemia cellsA polymerase inhibitor that binds to GC rich sequences located in the minor groove of DNA;DNA binding fluorescent dye. Until 2000 it was used to reduce high levels of plasma calcium; Used as an antineoplastic agent

Mithramycin A is an antibiotic DNA/RNA polymerase and DNA binding transcriptional inhibitor observed to facilitate TNF-α and Fas-ligand induced apoptosis. As a DNA binding transcriptional inhibitor, mithramycin A binds to GC rich sequences located in the minor groove of DNA and is noted to be reversible and Mg2+ dependent. Additionally reported to a block transcriptional activation of the SV40 promoter via competitive binding against Sp1 transcription factor to GC rich areas in the early promoter. Mithramycin A is noted to supress TNF-α induced expression of fractalkine (CX3CL1) mRNA in a dose-dependent manner and to act as an effective differentiation agent of HL60 promyelocytic leukemia cells
A polymerase inhibitor that binds to GC rich sequences located in the minor groove of DNA;DNA binding fluorescent dye. Until 2000 it was used to reduce high levels of plasma calcium; Used as an antineoplastic agent

纯度 ≥95%

关联靶点(人)

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活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DU-145 (51482 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PANC-1 (6144 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
A549 (127892 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HCT-116 (91556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prostatic carcinoma cell (85 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LNCaP (8286 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HeLa (62764 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DMS-114 (15429 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U-118-MG (352 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ES8 (149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ES7 (149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EWSR1 Tbio Friend leukemia integration 1 transcription factor (Proto-oncogene Fli-1)/RNA-binding protein EWS (19 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TC-32 (111 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
VCaP (1078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504757537
分子类型 小分子
IIUPAC Name (2S,3S)-2-[(2S,4R,5R,6R)-4-[(2S,4R,5S,6R)-4-[(2S,4S,5R,6R)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-5-hydroxy-6-methyloxan-2-yl]oxy-5-hydroxy-6-methyloxan-2-yl]oxy-3-[(1S,3S,4R)-3,4-dihydroxy-1-methoxy-2-oxopentyl]-6-[(2S,4R,5R,6R)-4-[(2S,4R,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-5-hydroxy-6-methyloxan-2-yl]oxy-8,9-dihydroxy-7-methyl-3,4-dihydro-2H-anthracen-1-one
INCHI 1S/C52H76O24/c1-18-29(72-34-14-30(43(58)21(4)68-34)73-33-13-28(54)42(57)20(3)67-33)12-26-10-25-11-27(49(66-9)48(63)41(56)19(2)53)50(47(62)39(25)46(61)38(26)40(18)55)76-36-16-31(44(59)23(6)70-36)74-35-15-32(45(60)22(5)69-35)75-37-17-52(8,65)51(64)24(7)71-37/h10,12,19-24,27-28,30-37,41-45,49-51,53-61,64-65H,11,13-17H2,1-9H3/t19-,20-,21-,22-,23-,24-,27+,28-,30-,31-,32-,33+,34+,35+,36+,37+,41+,42-,43-,44-,45+,49+,50+,51-,52+/m1/s1
InChi Key CFCUWKMKBJTWLW-BKHRDMLASA-N
Smiles CC1C(C(CC(O1)OC2CC(OC(C2O)C)OC3=CC4=CC5=C(C(=O)C(C(C5)C(C(=O)C(C(C)O)O)OC)OC6CC(C(C(O6)C)O)OC7CC(C(C(O7)C)O)OC8CC(C(C(O8)C)O)(C)O)C(=C4C(=C3C)O)O)O)O
Isomeric SMILES C[C@@H]1[C@H]([C@@H](C[C@@H](O1)O[C@@H]2C[C@@H](O[C@@H]([C@H]2O)C)OC3=CC4=CC5=C(C(=O)[C@H]([C@@H](C5)[C@@H](C(=O)[C@H]([C@@H](C)O)O)OC)O[C@H]6C[C@H]([C@@H]([C@H](O6)C)O)O[C@H]7C[C@H]([C@H]([C@H](O7)C)O)O[C@H]8C[C@]([C@@H]([C@H](O8)C)O)(C)O)C(=C4C(=C3C)O)O)O)O
UN Number 2811
分子量 1085.15
Beilstein号 5236667
Reaxy-Rn 24710368
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24710368&ln=

化学和物理性质

溶解性 Soluble in phosphate buffered saline (1 mg/ml), ethanol, ethyl acetate, lower alcohols, and acetone. Insoluble in water.
密度 1.48
敏感性 对光线和湿度敏感
熔点 170-175°C
分子量 1085.100 g/mol
XLogP3 0.600
氢键供体数Hydrogen Bond Donor Count 11
氢键受体数Hydrogen Bond Acceptor Count 24
可旋转键计数Rotatable Bond Count 15
精确质量Exact Mass 1084.47 Da
单同位素质量Monoisotopic Mass 1084.47 Da
拓扑极表面积Topological Polar Surface Area 358.000 Ų
重原子数Heavy Atom Count 76
形式电荷Formal Charge 0
复杂度Complexity 1940.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 25
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

象形图 GHS07
信号词 警告
危险声明

H302: 吞食有害

H361: 怀疑破坏生育力或未出生的孩子

预防措施声明

P264: 处理后要彻底洗手。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P330: 漱口

P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。

P308+P313: 如接触到或有疑虑:求医/就诊。

P501: 将内容物/容器处理到。。。

WGK Germany 3
RTECS PZ2800000
个人防护装备 dust mask type N95 (US),Eyeshields,Faceshields,Gloves

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找到8个结果

批号(Lot Number) 证书类型 货号
J2523005 分析证书 P113149
J2510048 分析证书 P113149
I2419126 分析证书 P113149
E2225243 分析证书 P113149
E2225244 分析证书 P113149
E2225253 分析证书 P113149
L2109072 分析证书 P113149
L2109073 分析证书 P113149

此产品的引用文献

引用文献

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21. Tsung-I Hsu,Mei-Chun Wang,Szu-Yu Chen,Shih-Ting Huang,Yu-Min Yeh,Wu-Chou Su,Wen-Chang Chang,Jan-Jong Hung.  (2012-09-08)  Betulinic acid decreases specificity protein 1 (Sp1) level via increasing the sumoylation of sp1 to inhibit lung cancer growth..  Molecular pharmacology,  82  ((6)): (1115-1128).  [PMID:22956772]
22. Carolina Vizcaíno,Sylvia Mansilla,Luz-Elena Núñez,Carmen Méndez,José A Salas,Francisco Morís,José Portugal.  (2012-09-18)  Novel mithramycins abrogate the involvement of protein factors in the transcription of cell cycle control genes..  Biochemical pharmacology,  84  ((9)): (1133-1142).  [PMID:22981341]
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25. Chun-Wei Hsu,Chia-Feng Kuo,Show-Mei Chuang,Ming-Hon Hou.  (2012-10-26)  Elucidation of the DNA-interacting properties and anticancer activity of a Ni(II)-coordinated mithramycin dimer complex..  Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine,  26  ((1)): (1-12).  [PMID:23097078]
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29. Valentina Sica,Jose Manuel Bravo-San Pedro,Valentina Izzo,Jonathan Pol,Sandra Pierredon,David Enot,Sylvère Durand,Noélie Bossut,Alexis Chery,Sylvie Souquere,Gerard Pierron,Evangelia Vartholomaiou,Naoufal Zamzami,Thierry Soussi,Allan Sauvat,Laura Mondragón,Oliver Kepp,Lorenzo Galluzzi,Jean-Claude Martinou,Holger Hess-Stumpp,Karl Ziegelbauer,Guido Kroemer,Maria Chiara Maiuri.  (2019-04-18)  Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate..  Cell reports,  27  ((3)): (820-834).  [PMID:30995479]
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31. Waise Quarni,Rinku Dutta,Ryan Green,Sandhyabanu Katiri,Bhaumik Patel,Shyam S Mohapatra,Subhra Mohapatra.  (2019-10-28)  Mithramycin A Inhibits Colorectal Cancer Growth by Targeting Cancer Stem Cells..  Scientific reports,  ((1)): (15202-15202).  [PMID:31645574]
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39. Eun-Sun Choi,Ji-Youn Jung,Jin-Seok Lee,Jong-Hwan Park,Nam-Pyo Cho,Sung-Dae Cho.  (2012-09-25)  Myeloid cell leukemia-1 is a key molecular target for mithramycin A-induced apoptosis in androgen-independent prostate cancer cells and a tumor xenograft animal model..  Cancer letters,  328  ((1)): (65-72).  [PMID:23000424]
40. Ji-Ae Shin,Ji-Youn Jung,Mi Heon Ryu,Stephen Safe,Sung-Dae Cho.  (2012-09-29)  Mithramycin A inhibits myeloid cell leukemia-1 to induce apoptosis in oral squamous cell carcinomas and tumor xenograft through activation of Bax and oligomerization..  Molecular pharmacology,  83  ((1)): (33-41).  [PMID:23019217]
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