| TBCACK2 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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| Cas No. | 934358-00-6 | SDF | Download SDF |
| Synonyms | Casein Kinase II Inhibitor III,Tetrabromocinnamic Acid | ||
| Chemical Name | (2E)-3-(2,3,4,5-tetrabromophenyl)-2-propenoic acid | ||
| Canonical SMILES | BrC1=C(Br)C(Br)=C(Br)C=C1/C=C/C(O)=O | ||
| Formula | C9H4Br4O2 | M.Wt | 463.7 |
| Solubility | ≤1mg/ml in ethanol;2mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline 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. | ||
Tetrabromocinnamic Acid (TBCA) is a new class of specific protein kinase CK2 inhibitors [1].
Protein kinases have been involved in catalyzing the phosphorylation of serine, threonine and tyrosine residues in protein substrates that play dominant roles in controlling nearly all cellular functions. The Ser/Thr-specific protein kinase CK2 has been implicated in signal transduction, gene expression, DNA repair, RNA and protein synthesis. CK2 is invariably elevated in a wide spectrum of tumours [1].
In vitro: TBCA was a selective, cell-permeable inhibitor of CK2 with an IC50 of 0.11 μM. The Ki value was 77 nM. TBCA showed minimal effect on a panel of 28 other kinases. TBCA induced cell death in Jurkat adult T cell leukemia cells with an DC50 of 7.7 μM [1]. TBCA dose-dependently inhibited platelet aggregation and secretion induced by various agonists including 2-MeSADP, AYPGKF, SFLLRN, and CRP [2]. TBCA also significantly inhibited agonist-induced thromboxane A2 (TxA2) generation and ERK phosphorylation. TBCA significantly inhibited platelet spreading on immobilized fibrinogen surface and clot retraction mediated by integrin αIIbβ3 signaling [2].
References:[1] Pagano M A, Poletto G, Di Maira G, et al. Tetrabromocinnamic acid (TBCA) and related compounds represent a new class of specific protein kinase CK2 inhibitors[J]. Chembiochem, 2007, 8(1): 129-139.[2] Ryu S Y, Kim S. Evaluation of CK2 inhibitor (E)-3-(2, 3, 4, 5-tetrabromophenyl) acrylic acid (TBCA) in regulation of platelet function[J]. European journal of pharmacology, 2013, 720(1): 391-400.
