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Oridonin/冬凌草甲素 {[allProObj[0].p_purity_real_show]}

货号:A472649 同义名: NSC-250682; Isodonol

Oridonin是一种抗肿瘤剂,是从红色马兜铃(Rabdosia rubescens)中纯化的二萜类化合物。Oridonin 通过共价键与 NLRP3 NACHT 域的半胱氨酸 279 发生反应,消除了 NLRP3-NEK7 的相互作用,抑制了随后的 NLRP3 炎症小体的激活。

Oridonin/冬凌草甲素 化学结构 CAS号:28957-04-2
Oridonin/冬凌草甲素 化学结构
CAS号:28957-04-2
Oridonin/冬凌草甲素 3D分子结构
CAS号:28957-04-2
Oridonin/冬凌草甲素 化学结构 CAS号:28957-04-2
Oridonin/冬凌草甲素 3D分子结构 CAS号:28957-04-2
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Oridonin/冬凌草甲素 纯度/质量文件 产品仅供科研

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产品名称 Akt Akt1 Akt2 Akt3 其他靶点 纯度
Honokiol MEK 98%
PF-04691502 ++++

P-Akt (T308), IC50: 7.5 nM

P-Akt (S473), IC50: 3.8 nM

98+%
PHT-427 +

Akt, Ki: 2.7 μM

99%+
Deguelin PI3K 99%+
TIC10 isomer ERK 98+%
Perifosine +

Akt, IC50: 4.7 μM

98%
Miltefosine PKC,PI3K 98%
Triciribine +

Akt, IC50: 130 nM

99%+
Uprosertib +

Akt1, IC50: 180 nM

+

Akt2, IC50: 328 nM

++

Akt3, IC50: 38 nM

99%+
Afuresertib ++++

Akt1, Ki: 0.08 nM

++++

Akt2, Ki: 2 nM

++++

Akt3, Ki: 2.6 nM

99%+
Miransertib ++++

Akt1, IC50: 5 nM

++++

Akt2, IC50: 4.5 nM

++

Akt3, IC50: 16 nM

98+%
GSK-690693 ++++

Akt1, IC50: 2 nM

+++

Akt2, IC50: 13 nM

+++

Akt3, IC50: 9 nM

99%+
AT7867 ++

Akt1, IC50: 32 nM

++

Akt2, IC50: 17 nM

++

Akt3, IC50: 47 nM

PKA 99%+
AKT inhibitor VIII ++

Akt1, IC50: 58 nM

+

Akt2, IC50: 210 nM

+

Akt3, IC50: 2119 nM

97%
MK-2206 2HCl +++

Akt1, IC50: 8 nM

+++

Akt2, IC50: 12 nM

+

Akt3, IC50: 65 nM

99%+
Ipatasertib ++++

Akt1, IC50: 5 nM

++

Akt2, IC50: 18 nM

+++

Akt3, IC50: 8 nM

99%+
AT13148 ++

Akt1, IC50: 38 nM

+

Akt2, IC50: 402 nM

++

Akt3, IC50: 50 nM

PKA 95%
Capivasertib ++++

Akt1, IC50: 3 nM

+++

Akt2, IC50: 8 nM

+++

Akt3, IC50: 8 nM

99%+
A-674563 HCl +++

Akt1, Ki: 11 nM

PKA 99%
CCT128930 +++

Akt2, IC50: 6 nM

PKA 95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Oridonin/冬凌草甲素 生物活性

描述 Oridonin, a diterpenoid isolated from medicinal herb Rabdosia rubescens, possesses potent antitumor effect. The IC50 values of Oridonin in MG-63, HOS, Saos-2 and U-2OS cells were 12.29 ± 1.02, 13.22 ± 0.86, 19.72 ± 0.75, and 19.56 ± 0.47 μM, respectively, after 24 h of treatment. In vitro, oridonin had a selectively inhibitory effect on osteosarcoma cells but not on normal cells[3]. In vivo, oridonin exhibited potent inhibitory effects in both WT and mutated HL60/p210 clones[6].

Oridonin/冬凌草甲素 参考文献

[1]Ikezoe T, Yang Y, et al. Oridonin, a diterpenoid purified from Rabdosia rubescens, inhibits the proliferation of cells from lymphoid malignancies in association with blockade of the NF-kappa B signal pathways. Mol Cancer Ther. 2005 Apr;4(4):578-86.

[2]Ikezoe T, Chen SS, et al. Oridonin induces growth inhibition and apoptosis of a variety of human cancer cells. Int J Oncol. 2003 Oct;23(4):1187-93.

[3]Lu Y, Sun Y, Zhu J, Yu L, Jiang X, Zhang J, Dong X, Ma B, Zhang Q. Oridonin exerts anticancer effect on osteosarcoma by activating PPAR-γ and inhibiting Nrf2 pathway. Cell Death Dis. 2018 Jan 11;9(1):15. doi: 10.1038/s41419-017-0031-6. PMID: 29323103; PMCID: PMC5849031.

[4]Shi M, Lu XJ, Zhang J, et al. Oridonin, a novel lysine acetyltransferases inhibitor, inhibits proliferation and induces apoptosis in gastric cancer cells through p53- and caspase-3-mediated mechanisms. Oncotarget. 2016;7(16):22623-22631.

[5]He H, Jiang H, Chen Y, et al. Oridonin is a covalent NLRP3 inhibitor with strong anti-inflammasome activity. Nat Commun. 2018;9(1):2550. Published 2018 Jun 29.

[6]Huang H, Weng H, Dong B, Zhao P, Zhou H, Qu L. Oridonin Triggers Chaperon-mediated Proteasomal Degradation of BCR-ABL in Leukemia. Sci Rep. 2017 Jan 27;7:41525. doi: 10.1038/srep41525. PMID: 28128329; PMCID: PMC5270248.

Oridonin/冬凌草甲素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL

Oridonin/冬凌草甲素 技术信息

CAS号28957-04-2
分子式C20H28O6
分子量 364.43
SMILES Code O[C@]12[C@]34[C@](CC[C@](C(C4=O)=C)([H])C3O)([H])[C@@]5(CO2)C(C(C)(CC[C@H]5O)C)([H])[C@@H]1O
MDL No. MFCD00221762
别名 NSC-250682; Isodonol; Oridonine; Rubescenin
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案

DMSO: 60 mg/mL(164.64 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

5% DMSO+20%PEG 300+water 12.5 mg/mL

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