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| BVT 948PTPs inhibitor,cell-permeable and non-competitve |
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
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Cas No. | 39674-97-0 | SDF | Download SDF |
| Chemical Name | 3,3-dimethyl-1H-benzo[g]indole-2,4,5-trione | ||
| Canonical SMILES | CC1(C2=C(C3=CC=CC=C3C(=O)C2=O)NC1=O)C | ||
| Formula | C14H11NO3 | M.Wt | 241.25 |
| Solubility | Soluble in DMSO | Storage | Store at RT |
| 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. | ||
BVT948 is a noncompetitive, cell-permeable and novel PTP inhibitor with an IC50 of 0.09-1.7 µM. [1]
Protein-tyrosine phosphatases (PTPs) are involved in the regulation of diverse intracellular signalings. It can promote cell migration in mammalian cells [2], induce MMP-9 expression in MCF-7 breast cancer cells. [3]
BVT948 blocks breast cancer cell invasion via suppression of the expression of MMP-9. Treatment of 0.5, 1 or 5 μM BVT948 for 24 h did not cause any significant changes in MCF-7 cell viability. BVT948 inhibited TPA-induced MMP-9 up-regulation in a dose-dependent manner. Treatment MCF-7 cells with BVT948 blocked the up-regulation of TPA-induced MMP-9 protein expression. BVT948 significantly diminished TPA-induced MMP-9 secretion. BVT948 diminished 50% cell invasion after the TPA-induced. BVT948 inhibits NF-κB activation by suppressing IκBα degradation and the nuclear translocation of NF-κB in TPA-treated MCF-7 cells. The MAPK pathways are not involved in the inhibition of TPA-induced MMP-9 expression by BVT948. [4]
References:1.Liljebris, C., Baranczewski, P., Björkstrand, E., et al. Oxidation of protein tyrosine phosphatases as a pharmaceutical mechanism of action: A study using 4-hydroxy-3,3-dimethyl-2H-benzo [g]indole-2,5(3H)-dione.J Pharmacol Exp Ther 309(2) 711-719 (2004).2. Jallal, B., Mossie, K., Vasiloudis, G., Knyazev, P., Zachwieja, J., Clairvoyant, F., Schilling, J. and Ullrich, A. (1997) The receptor-like protein-tyrosine phosphatase DEP-1 is constitutively associated with a 64-kDa protein serine/threonine kinase. J. Biol. Chem. 272, 12158-12163.3. Wang, F. M., Liu, H. Q., Liu, S. R., Tang, S. P., Yang, L. and Feng, G. S. (2005) SHP-2 promoting migration and metastasis of MCF-7 with loss of E-cadherin, dephosphorylation of FAK and secretion of MMP-9 induced by IL-1 beta in vivo and in vitro. Breast Cancer Res. Treat. 89, 5-14.4. Hwang BM, Chae HS, Jeong YJ et al.Protein tyrosine phosphatase controls breast cancer invasion through the expression of matrix metalloproteinase-9.BMB Rep. 2013 Nov;46(11):533-8.
