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曲西瑞宾

选择性，有效的Akt激活抑制剂
4篇引用文献 COA COA
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货号 (SKU) 包装规格 是否现货 价格 数量
T126748-5mg
 5mg 现货 Stock Image
T126748-10mg
 10mg 现货 Stock Image
T126748-25mg
 25mg 现货 Stock Image
T126748-50mg
 50mg 现货 Stock Image
T126748-100mg
 100mg 现货 Stock Image
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查看相关系列
Akt (179) Anti-infection (2804) Cell Cycle (7376) Cell Cycle/DNA Damage (2603) DNA/RNA Synthesis (362) HIV (248) PI3K/Akt/mTOR (764) Virus (3767)
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基本描述

别名 Akt/PKB信号传导抑制剂2 | 抑制剂 V | 曲西立滨
英文别名 AC-32686 | API-2 | Triciribine | Triciribine [INN] | UNII-2421HMY9N6 | AKOS024456958 | BiomolKI2_000078 | 1,4,5,6,8-Pentaazaacenaphthylene, 3-amino-1,5-dihydro-5-methyl-1-beta-D-ribofuranosyl- | TCN | BRD-K80431395-001-09-9 | HMS3413I03 | DB12405 | MLS006
规格或纯度 Moligand™, ≥99%
英文名称 Triciribine
生化机理 曲昔利宾又称 API-2，可抑制 Akt 的磷酸化水平和激酶活性。特瑞昔宾是一种细胞渗透性三环核苷，可抑制 Akt-1、-2 和-3 的磷酸化、激活和信号传导。 特瑞昔宾不抑制 Akt 的直接上游激活剂 PI3-Kinase 或 PDK1，也不抑制 PKC、PKA、ERK1/2、血清和糖皮质激素诱导激酶、p38、STAT3 或 JNK 信号通路。特瑞昔宾在体外诱导细胞凋亡和生长停滞，尤其适用于 Akt 水平升高的人类癌细胞。曲昔利宾能有效并选择性地抑制小鼠体内表达 Akt 的肿瘤的生长。细胞渗透性三环核苷可抑制 Akt 的磷酸化、激活和信号传导。对 PKC、PKA、SGK 和 p38 通路具有选择性。在体外诱导细胞生长停滞和凋亡。
储存温度 -20°C储存
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

Triciribine 是一种 DNA 合成 (DNA synthesis) 抑制剂，也抑制 Akt 和 HIV-1/2，IC50 分别为 130 nM 和 0.02-0.46 μM。
纯度 ≥99%

关联靶点（人）

ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOB Tclin Monoamine oxidase B (8835 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DAPK3 Tchem Death-associated protein kinase 3 (2108 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR2 Tclin Fibroblast growth factor receptor 2 (3405 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMK2B Tchem CaM kinase II beta (1626 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IKBKB Tchem Inhibitor of nuclear factor kappa B kinase beta subunit (5554 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DAPK2 Tchem Death-associated protein kinase 2 (740 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCE Tchem Protein kinase C epsilon (1520 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCG Tchem Protein kinase C gamma (2471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PRKD1 Tchem Protein kinase C mu (1904 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ITK Tclin Tyrosine-protein kinase ITK/TSK (3699 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CAMK1 Tchem CaM kinase I alpha (1664 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

pol Human immunodeficiency virus type 1 reverse transcriptase (18245 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr4 Fibroblast growth factor receptor 4 (138 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human betaherpesvirus 5 (5122 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human alphaherpesvirus 1 (11089 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus 1 (70413 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Simian immunodeficiency virus (338 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus 2 (5592 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus (3636 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
L1210 (27553 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FTL Ferritin light chain (43324 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 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 504753982
分子类型 小分子
IIUPAC Name (2R,3R,4S,5R)-2-(5-amino-7-methyl-2,6,7,9,11-pentazatricyclo[6.3.1.04,12]dodeca-1(12),3,5,8,10-pentaen-2-yl)-5-(hydroxymethyl)oxolane-3,4-diol
INCHI 1S/C13H16N6O4/c1-18-11-7-5(10(14)17-18)2-19(12(7)16-4-15-11)13-9(22)8(21)6(3-20)23-13/h2,4,6,8-9,13,20-22H,3H2,1H3,(H2,14,17)/t6-,8-,9-,13-/m1/s1
InChi Key HOGVTUZUJGHKPL-HTVVRFAVSA-N
Smiles CN1C2=NC=NC3=C2C(=CN3C4C(C(C(O4)CO)O)O)C(=N1)N
Isomeric SMILES CN1C2=NC=NC3=C2C(=CN3[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)C(=N1)N
PubChem CID 65399
分子量 320.3

化学和物理性质

溶解性 DMSO 64 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
分子量 320.300 g/mol
XLogP3 -1.600
氢键供体数Hydrogen Bond Donor Count 4
氢键受体数Hydrogen Bond Acceptor Count 8
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 320.123 Da
单同位素质量Monoisotopic Mass 320.123 Da
拓扑极表面积Topological Polar Surface Area 142.000 Ų
重原子数Heavy Atom Count 23
形式电荷Formal Charge 0
复杂度Complexity 507.000
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 4
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

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C of A & Other Certificates(BSE/TSE, COO):
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找到6个结果

批号(Lot Number) 证书类型 货号
K2229778 分析证书 T126748
K2229792 分析证书 T126748
K2229848 分析证书 T126748
K2229492 分析证书 T126748
K2229665 分析证书 T126748
K2229666 分析证书 T126748

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引用文献

1. Yang L, Dan HC, Sun M, Liu Q, Sun XM, Feldman RI, Hamilton AD, Polokoff M, Nicosia SV, Herlyn M et al..  (2004)  Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt..  Cancer Res,  64  (13): (4394-9).  [PMID:15231645]
2. Gürsel DB, Connell-Albert YS, Tuskan RG, Anastassiadis T, Walrath JC, Hawes JJ, Amlin-Van Schaick JC, Reilly KM.  (2011)  Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies..  Neuro-oncology,  13  (6): (610-21).  [PMID:21636709]
3. Wotring LL, Townsend LB, Jones LM, Borysko KZ, Gildersleeve DL, Parker WB.  (1990)  Dual mechanisms of inhibition of DNA synthesis by triciribine..  Cancer Res,  50  (16): (4891-9).  [PMID:2379153]
4. Ptak RG, Borysko KZ, Porcari AR, Buthod JL, Holland LE, Shipman Jr C, Townsend LB, Drach JC.  (1998)  Phosphorylation of triciribine is necessary for activity against HIV type 1..  AIDS Res Hum Retroviruses,  14  (15): (1315-22).  [PMID:9788672]
5. Congyu Zhang, Wei-Hsin Chen, Shih-Hsin Ho, Anh Tuan Hoang, Ying Zhang.  (2023)  Tetracycline-adsorbed biochar for solid biofuel usage to achieve waste utilization for environmental sustainability.  ENVIRONMENTAL RESEARCH,  237  (116959).  [PMID:37619628] [10.1016/j.envres.2023.116959]
6. Kainan Zhang, Xinjie Cai, Yaru Guo, Chuanzi Liu, Tao Jiang, Yining Wang.  (2020)  Validation of the laser-induced fluorescence effect of aromatic amino acids, protoporphyrin IX, and tetracycline hydrochloride on hydroxyapatite.  JOURNAL OF RAMAN SPECTROSCOPY,  51  (12): (2447-2457).  [10.1002/jrs.6001]
7. Zhipeng Liao, Minh Nhat Nguyen, Gaojie Wan, Jia Xie, Linhan Ni, Junwen Qi, Jiansheng Li, Andrea Iris Schäfer.  (2020)  Low pressure operated ultrafiltration membrane with integration of hollow mesoporous carbon nanospheres for effective removal of micropollutants.  JOURNAL OF HAZARDOUS MATERIALS,  397  (122779).  [PMID:32387831] [10.1016/j.jhazmat.2020.122779]
8. Wenquan Sun, Yiming Xie, Ming Zhang, Jun Zhou, Yongjun Sun.  (2024)  Preparation of Co–Ce@RM catalysts for catalytic ozonation of tetracycline.  WATER ENVIRONMENT RESEARCH,  96  (10): (e11146).  [PMID:39434465] [10.1002/wer.11146]

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