OSU-03012 (AR-12)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
OSU-03012（AR-12）是3-磷酸肌醇依赖性激酶-1（PDK-1）的抑制剂，IC50值为5 μM。抑制效能比OSU-02067高2倍[1]。
在PC-3细胞中，OSU-03012抑制PC-3细胞的增殖和诱导细胞凋亡。PDK-1和Akt组成型活性形式的表达可减少OSU-03012诱导的细胞凋亡[1]。
OSU-03012以剂量依赖的方式有效抑制原代人VS细胞和恶性神经鞘瘤HMS-97细胞的生长。而正常的人Schwann细胞对OSU-03012有抵抗力。此外，在VS和HMS-97细胞中，OSU-03012抑制Akt苏氨酸308位点的磷酸化[2]。
参考文献：
[1] Zhu J1,?Huang JW,?Tseng PH,?Yang YT,?Fowble J,?Shiau CW,?Shaw YJ,?Kulp SK,?Chen CS. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res.?2004 Jun 15;64(12):4309-18.
[2] Lee TX1,?Packer MD,?Huang J,?Akhmametyeva EM,?Kulp SK,?Chen CS,?Giovannini M,?Jacob A,?Welling DB,?Chang LS. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer.?2009 Jun;45(9):1709-20.?
- 1. Daphne R. Mattos, Marcus A. Weinman, et al. "Canine osteosarcoma cells exhibit basal accumulation of multiple chaperone proteins and are sensitive to small molecule inhibitors of GRP78 and heat shock protein function." Cell Stress Chaperones. 2022 May;27(3):223-239. PMID: 35244890
- 2. Dr Jason King. "Katnip, a novel microtubule and autophagy regulator." University of Sheffield December 2020.
- 3. Rausch JL, Boichuk S, et al. "Opposing roles of KIT and ABL1 in the therapeutic response of gastrointestinal stromal tumor (GIST) cells to imatinib mesylate." Oncotarget. 2017 Jan 17;8(3):4471-4483. PMID: 27965460
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 460.45 |
| Cas No. | 742112-33-0 |
| Formula | C26H19F3N4O |
| Solubility | ≥23 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
|
细胞系 |
PC-3 (p53-/-)人类雄激素非反应性前列腺癌细胞 |
|
溶解方法 |
在DMSO中的溶解度>23mg/mL。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
1、2.5、5、7.5、10 μM; 6 h |
|
应用 |
在PC-3 (p53-/-)人类雄激素非反应性前列腺癌细胞中，OSU-03012以剂量依赖的方式降低免疫沉淀的p70S6K的活性。 亚μM浓度范围的OSU-03012在抑制PC-3细胞增殖方面是有效的。 |
| 动物实验[2]: | |
|
动物模型 |
皮下移植Huh7肿瘤异种移植物的裸鼠 |
|
剂量 |
100和200 mg/kg，给药28天，灌胃 |
|
应用 |
在皮下移植Huh7肿瘤异种移植物的裸鼠中，OSU-03012（100和200mg/kg，28天）分别抑制39.52％和57.59％的Huh7肿瘤生长。与对照相比，OSU-03012显著减少肿瘤体积。OSU-03012在异种移植物中诱导自噬。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Zhu J1, Huang JW, Tseng PH, Yang YT, Fowble J, Shiau CW, Shaw YJ, Kulp SK, Chen CS. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 2004 Jun 15;64(12):4309-18. [2] Lee TX1, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20. |
|
| 描述 | OSU-03012是重组PDK-1的高效抑制剂，IC50值为5 μM。 | |||||
| 靶点 | recombinant PDK-1 | |||||
| IC50 | 5 μM | |||||
质量控制和MSDS
- 批次:
化学结构
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