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| A 205804E-selectin/ICAM-1 expression 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 = 98.29%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
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- Datasheet
Chemical structure
| Description | A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 values of 20 nM and 25 nM, respectively. | |||||
| Targets | E-selectin | ICAM-1 | ||||
| IC50 | 20 nM | 25 nM | ||||
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| Cas No. | 251992-66-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide | ||
| Canonical SMILES | CC1=CC=C(C=C1)SC2=C3C=C(SC3=CN=C2)C(=O)N | ||
| Formula | C15H12N2OS2 | M.Wt | 300.39 |
| Solubility | ≥30mg/mL in DMSO | 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. | ||
A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 value of 20 nM and 25 nM, respectively [1].
E-selectin is a cell adhesion molecule and plays an important role in recruiting leukocytes to injury site during inflammation process. ICAM-1 (intracellular adhesion molecule 1) is a ligand for LFA-1 and involves in leukocytes binding to endothelial cells process. It has been reported that abnormal expression of E-selectin and ICAM-1 are correlated with a variety of cancers [2].
A-205804 is a selective E-selectin and ICAM-1 inhibitor over VCAM-1. When tested with primary HUVECs cells, A-205804 treatment reduced cell migration ability by inhibiting the expression of E-selectin and ICAM-1 [3]. In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations [1]. Further, it was revealed that A-205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs) [4].
References: [1]. Stewart, A.O., et al., Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem, 2001. 44(6): p. 988-1002.[2]. Chang, C.Z., et al., Valproic acid attenuates intercellular adhesion molecule-1 and E-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. J Inflamm (Lond), 2015. 12: p. 27.[3]. Zhu, G.D., et al., Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem, 2001. 44(21): p. 3469-87. [4]. Zhu, G.D., et al., Synthesis and mode of action of (125)I- and (3)H-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. J Org Chem, 2002. 67(3): p. 943-8.
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最近遇到了实验上的大问题，就是用一步法做RNA的荧光定量PCR时，发现低浓度的做不出来，而DNA是可以的，想请问各位在一步法PCR中有没有什么高见，就是逆转录的Buffer有没有什么需要注意的地方！就是在逆转录酶的最适Buffer和Taq酶的最适Buffer中寻找一个最适的Buffer！
DNA拓扑异构酶Ⅱ与抗肿瘤药物靶点的研究进展.doc(59.5k)
B、酶细胞产能细胞内（外）起作用消化酶细胞外起作用B错误；
C、酶同需要适条件同胃蛋白酶与胰蛋白酶所需PH同C错误；
D、葡萄糖细胞质基质解丙酮酸需要酶催化D确．
故选：D．
我是新手。我要开始做实验了，但一开始就碰到了个很大的问题。
我想买个能利用哺乳动物细胞RNA聚合酶将DNA转录成RNA的的质粒，向好几家公司打了电话，但都没有我想要的东西。
没有这个东西，我的实验就只能是蓝图了。哪位战友有办法的，能不能帮帮我？
不胜感激。
请规范发贴，求助贴请在标题前加【求助】，谢谢您的合作。——by草根
