| 词条 | K252a |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 461783276 | ImageFile=(+)-K252a.svg | ImageFile2=(+)-K252a 1R0P.png | ImageSize= | IUPACName= (9S-(9α,10β,12α))-2,3,9,10,11,12-hexahydro-10-hydroxy-10-(methoxycarbonyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one | OtherNames= |Section1={{Chembox Identifiers | CASNo_Ref = {{cascite|changed|??}} | CASNo=99533-80-9 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 2299962 | PubChem=3035817 | IUPHAR_ligand = 336 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 281948 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = IV7H45AM5B | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C27H21N3O5/c1-26-27(33,25(32)34-2)11-18(35-26)29-16-9-5-3-7-13(16)20-21-15(12-28-24(21)31)19-14-8-4-6-10-17(14)30(26)23(19)22(20)29/h3-10,18,33H,11-12H2,1-2H3,(H,28,31)/t18?,26-,27-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = KOZFSFOOLUUIGY-CYBHFKQVSA-N | SMILES= |Section2={{Chembox Properties | Properties_ref = [1] | C=27 | H=21 | N=3 | O=5 | MolarMass= | Appearance= | Density= | MeltingPt= | BoilingPt= | Solubility= | SolubleOther = Soluble in DMSO, dichloromethane, and methanol | Solvent = other solvents |Section3={{Chembox Hazards | MainHazards= | FlashPt= | AutoignitionPt = }}K252a is an alkaloid isolated from Nocardiopsis bacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).[2][3][4][5][6][7][8][9] K252a is reported to promote myogenic differentiation in C2 mouse myoblasts[6] and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.[10] K252a has been reported in preclinical research as a potential treatment for psoriasis [11] K252a inhibits tyrosine phosphorylation of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 10 ng/ml NGF with or without various concentrations of K252a. See also
References1. ^K252a from Fermentek 2. ^Ruegg, U.T. et al. (1989) Tips 10, 218. 3. ^Eliot, L.H. et al. (1990) B.B.R.C. 171, 148. 4. ^Simpson, D.l. et al. (1991) J. Neurosci. Res, 28, 148. 5. ^Chin, L.S. et al. (1999) Cancer Invest. 17, 391. 6. ^1 Tapley, P. et al. (1992) Oncogene 7, 371. 7. ^Hashimoto, S. (1998) J. Cell Biol. 107, 1531. 8. ^Kase, H. et al. (1987) B.B.R.C. 142, 436. 9. ^Hirayama E. et al. (2001) B.B.R.C. 285, 1237. 10. ^Borasio, G.D. Neurosci. Lett. (1990) 108, 207. 11. ^Promising New Treatments for Psoriasis, Sarah Dubois Declercq and Roxane Pouliot >. The Scientific World Journal; Volume 2013, Article ID 980419; https://dx.doi.org/10.1155/2013/980419 Further reading
|vauthors=Wood JL, Stoltz BM, Dietrich HJ | journal = J Am Chem Soc | year = 1995 | volume = 117 | issue = 41 | pages = 10413–4 |doi=10.1021/ja00146a039}}{{Growth factor receptor modulators}}{{biochem-stub}} 7 : Alkaloids|Indolocarbazoles|Lactams|Protein kinase inhibitors|TrkB antagonists|Alcohols|Methyl esters |
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