For research use only. Not for therapeutic Use.
Lavendustin C, also known as HDBA and NSC 666251, is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with an IC50 value of 0.012 µM.. HDBA inhibits tyrosine kinase-associated neutrophil degranulation and superoxide generation
Catalog Number | R000086 |
CAS Number | 125697-93-0 |
Synonyms | Lavendustin C; NSC 666251; |
Molecular Formula | C14H13NO5 |
Purity | ≥95% |
Target | Protein Tyrosine Kinase/RTK |
Solubility | Soluble in DMSO |
Storage | Store at -20°C |
IUPAC Name | 5-[(2,5-dihydroxyphenyl)methylamino]-2-hydroxybenzoic acid |
InChI | InChI=1S/C14H13NO5/c16-10-2-4-12(17)8(5-10)7-15-9-1-3-13(18)11(6-9)14(19)20/h1-6,15-18H,7H2,(H,19,20) |
InChIKey | LULATDWLDJOKCX-UHFFFAOYSA-N |
SMILES | C1=CC(=C(C=C1NCC2=C(C=CC(=C2)O)O)C(=O)O)O |
Reference | </br>1: Nynca A, Nynca J, Wąsowska B, Kolesarova A, Kołomycka A, Ciereszko RE. Effects of the phytoestrogen, genistein, and protein tyrosine kinase inhibitor-dependent mechanisms on steroidogenesis and estrogen receptor expression in porcine granulosa cells of medium follicles. Domest Anim Endocrinol. 2013 Jan;44(1):10-8. doi: 10.1016/j.domaniend.2012.07.002. Epub 2012 Aug 10. PubMed PMID: 22920265.</br> 2: Kobayashi T, Nemoto S, Ishida K, Taguchi K, Matsumoto T, Kamata K. Involvement of CaM kinase II in the impairment of endothelial function and eNOS activity in aortas of Type 2 diabetic rats. Clin Sci (Lond). 2012 Sep;123(6):375-86. doi: 10.1042/CS20110621. PubMed PMID: 22494112.</br> 3: Opałka M, Kamińska B, Ciereszko R, Dusza L. Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus). Reprod Biol. 2004 Jul;4(2):185-93. PubMed PMID: 15297892.</br> 4: Nynca A, Sadowska A, Orlowska K, Jablonska M, Ciereszko RE. The Effects of Phytoestrogen Genistein on Steroidogenesis and Estrogen Receptor Expression in Porcine Granulosa Cells of Large Follicles. Folia Biol (Krakow). 2015;63(2):119-28. PubMed PMID: 26255463.</br> 5: Watanabe H, Takahashi R, Tran QK, Takeuchi K, Kosuge K, Satoh H, Uehara A, Terada H, Hayashi H, Ohno R, Ohashi K. Increased cytosolic Ca(2+) concentration in endothelial cells by calmodulin antagonists. Biochem Biophys Res Commun. 1999 Nov 30;265(3):697-702. PubMed PMID: 10600483.</br> 6: Agbotounou WK, Umezawa K, Jacquemin-Sablon A, Pierre J. Inhibition by two lavendustins of the tyrosine kinase activity of pp60F527 in vitro and in intact cells. Eur J Pharmacol. 1994 Sep 15;269(1):1-8. PubMed PMID: 7828651.</br> 7: Lavens-Phillips SE, Mockford EH, Warner JA. The effect of tyrosine kinase inhibitors on IgE-mediated histamine release from human lung mast cells and basophils. Inflamm Res. 1998 Mar;47(3):137-43. PubMed PMID: 9562339.</br> 8: Yoon J, Ryu JS. A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly. Bioorg Med Chem Lett. 2010 Jul 1;20(13):3930-5. doi: 10.1016/j.bmcl.2010.05.014. Epub 2010 May 12. PubMed PMID: 20570145.</br> 9: Lidington D, Ouellette Y, Tyml K. Endotoxin increases intercellular resistance in microvascular endothelial cells by a tyrosine kinase pathway. J Cell Physiol. 2000 Oct;185(1):117-25. PubMed PMID: 10942525.</br> 10: Li B. [Construction of a three-dimensional human angiogenesis model in vitro for antiangiogenic drug selection]. Di Yi Jun Yi Da Xue Xue Bao. 2004 Oct;24(10):1167-70. Chinese. PubMed PMID: 15485791.</br> 11: Burt HM, Jackson JK, Salari H. Inhibition of crystal-induced neutrophil activation by a protein tyrosine kinase inhibitor. J Leukoc Biol. 1994 Jan;55(1):112-9. PubMed PMID: 8283135.</br> 12: Valle-Aviles L, Valentin-Berrios S, Gonzalez-Mendez RR, Rodriguez-Del Valle N. Functional, genetic and bioinformatic characterization of a calcium/calmodulin kinase gene in Sporothrix schenckii. BMC Microbiol. 2007 Nov 29;7:107. PubMed PMID: 18047672; PubMed Central PMCID: PMC2242797.</br> 13: Bai GY, Piao FL, Kim SY, Yuan K, Kim SZ, Kim SH. Augmentation of insulin-stimulated ANP release through tyrosine kinase and PI 3-kinase in diabetic rats. Peptides. 2006 Nov;27(11):2756-63. Epub 2006 Jul 10. PubMed PMID: 16828931.</br> 14: Schneider JC, El Kebir D, Chéreau C, Lanone S, Huang XL, De Buys Roessingh AS, Mercier JC, Dall/’Ava-Santucci J, Dinh-Xuan AT. Involvement of Ca2+/calmodulin-dependent protein kinase II in endothelial NO production and endothelium-dependent relaxation. Am J Physiol Heart Circ Physiol. 2003 Jun;284(6):H2311-9. Epub 2003 Jan 30. PubMed PMID: 12560211.</br> 15: Zucchi R, Ghelardoni S, Carnicelli V, Frascarelli S, Ronca F, Ronca-Testoni S. Ca2+ channel remodeling in perfused heart: Effects of mechanical work and interventions affecting Ca2+ cycling on sarcolemmal and sarcoplasmic reticulum Ca2+ channels. FASEB J. 2002 Dec;16(14):1976-8. Epub 2002 Oct 18. PubMed PMID: 12397086.</br> 16: Wang Z, Wilson GF, Griffith LC. Calcium/calmodulin-dependent protein kinase II phosphorylates and regulates the Drosophila eag potassium channel. J Biol Chem. 2002 Jul 5;277(27):24022-9. Epub 2002 Apr 29. PubMed PMID: 11980904.</br> 17: Taybi T, Cushman JC. Signaling events leading to crassulacean acid metabolism induction in the common ice plant. Plant Physiol. 1999 Oct;121(2):545-56. PubMed PMID: 10517846; PubMed Central PMCID: PMC59417.</br> 18: Imoto M, Sujikai I, Ui H, Umezawa K. Involvement of tyrosine kinase in growth factor-induced phospholipase C activation in NIH3T3 cells. Biochim Biophys Acta. 1993 Feb 24;1166(2-3):188-92. PubMed PMID: 8443236.</br></br></br> |