- U 73343
- U-73122
- RHC 80267
| D609PC-PLC inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
Related Biological Data
| Description | D609 is an inhibitor of phosphatidylcholine specific phospholipase C (PC-PLC) with IC50 values of 94 µM. | |||||
| Targets | PC-PLC | |||||
| IC50 | 94 µM | |||||
| Cell experiment [1]: | |
Cell lines | HER2-overexpressing SKBr3 cells and various cancer cells |
Preparation method | The solubility of this compound in DMSO is > 12.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | 50 μg/mL |
Applications | D609 inhibited PC-PLC, which enhanced HER2 internalization and lysosomal degradation, inducing down-regulation of HER2 expression on the membrane. Moreover, D609-induced PC-PLC inhibition significantly delayed HER2 re-expression on the membrane and reduced the overall cellular contents of HER2, HER2-HER3 and HER2-EGFR heterodimers. In addition, D609 also exhibited antiproliferative effects, especially in Trastuzumab-resistant cells, via PC-PLC inhibition. In breast cancer cells, D609 at the dose of 50 μg/mL decreased the activity of PC-PLC by 3.5 folds within 1hr. |
References: [1]. Paris L, Cecchetti S, Spadaro F, Abalsamo L, Lugini L, Pisanu ME, Iorio E, Natali PG, Ramoni C, Podo F. Inhibition of phosphatidylcholine-specific phospholipase C downregulates HER2 overexpression on plasma membrane of breast cancer cells. Breast Cancer Res. 2010;12(3):R27. | |
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| Cas No. | 83373-60-8 | SDF | Download SDF |
| Synonyms | D-609 potassium, D 609, D-609 | ||
| Chemical Name | potassium O-(octahydro-1H-4,7-methanoinden-5-yl) carbonodithioate | ||
| Canonical SMILES | S=C(S[K])OC1CC2C3C(CCC3)C1C2 | ||
| Formula | C11H15KOS2 | M.Wt | 266.47 |
| Solubility | ≥35.33 mg/mL in DMSO with gentle warming, ≥24.5 mg/mL in EtOH with ultrasonic and warming, ≥12.7 mg/mL in H2O | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
D609 is a specific and competitive inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC) with a Ki value of 6.4 μM. [1]
PC-PLC hydrolyzes (phosphatidylcholine) PC to generate 1, 2-diacylglycerol (DAG) and phosphocholine. D609 is a widely known inhibitor of PC-PLC and also inhibit sphingomyelin synthase (SMS). Due to these actions, it has antiviral and antitumor properties. D609 does not inhibit bacterial phosphatidylinositol (PI)-PLC, bovine pancreatic PLA2 or phospholipase D from cabbage[1b]. In OVCAR3 cells treated with (53 μg/mL) for 24 h, PC-PLC activity was significantly inhibited and cell proliferation was affected. In breast cancer cells, the activity of PC-PLC decreased 3.5 fold after the incubation with D609 (50 μg/ml) within 1h. The human epidermal growth factor receptor 2 (HER2) was also down-regulated [2]. D609 also has anti-inflammatory functions. It blocked the nitric oxide synthase induced by LPS (IC50=20 μg/mL) and IL-1β induced vascular cell adhesion molecule 1 gene expression in human endothelial cells.[3]
D609 can reduce sphingomyelin synthase, thereby it inhibits bFGF-stimulated astrocyte proliferation. Because of the presence of the thiol function, D609 also has antioxidant/glutathione mimetic properties[1b].
References:1.a) E. Amtmann, Drugs Exp Clin Res 1996, 22, 287-294; b) R. M. Adibhatla, J. F. Hatcher and A. Gusain, Neurochem Res 2012, 37, 671-679. 2.L. Paris, S. Cecchetti, F. Spadaro, L. Abalsamo, L. Lugini, M. E. Pisanu, E. Iorio, P. G. Natali, C. Ramoni and F. Podo, Breast Cancer Res 2010, 12, R27. 3.a) K. Tschaikowsky, M. Meisner, F. Schonhuber and E. Rugheimer, Br J Pharmacol 1994, 113, 664-668; b) R. R. Cobb, K. A. Felts, G. C. Parry and N. Mackman, Mol Pharmacol 1996, 49, 998-1004.
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我在做5RACE,选用TaKaRa公司的RNA反转录酶（RNaseH-），不知道这个酶好不好，有什么需要注意的。
没有序列识别的功能，他就是简单的催化相邻DNA链的5-P末端和3'-OH末端以磷酸二酯键结合的反应，需ATP作辅酶。 不仅可以催化粘性末端之间或平滑末端之间的DNA的连接，也催化DNA与RNA之间以及少数RNA之间的连接。
反转录酶（Reversetranscripatase）是以RNA为模板指导三磷酸脱氧核苷酸合成互补DNA（cDNA）的酶。哺乳类C型病毒的反转录酶和鼠类B型病毒的反转录酶都是一条多肽链。鸟类RNA病毒的反转录酶则由两上亚基结构。真核生物中也都分离出具有不同结构的反转录酶。
