K-252A
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- CAS-Nr.
- 99533-80-9
- Englisch Name:
- K-252A
- Synonyma:
- PROTEIN KINASE INHIBITOR;sf2370;K-252A;antibiotick252a;K 252a(SF 2370);antibioticsf2370;K-252A, NOCARDIOPSIS SP;(9-alpha,10-beta,12-alpha)-este;PROTEIN KINASE INHIBITOR K-252A;J61687 Protein Kinase Inhibitor K252A
- CBNumber:
- CB9493885
- Summenformel:
- C27H21N3O5
- Molgewicht:
- 467.47
- MOL-Datei:
- 99533-80-9.mol
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K-252A Eigenschaften
- Schmelzpunkt:
- 262-273℃ (decomposition) (methanol )
- Siedepunkt:
- 685.3±55.0 °C(Predicted)
- Dichte
- 1.68
- Flammpunkt:
- 87℃
- storage temp.
- -20°C
- L?slichkeit
- DMF: 1 mg/mL
- pka
- 11.95±0.40(Predicted)
- Aggregatzustand
- Lyophilized solid.
- Farbe
- White or off-white
- Biologische Quelle
- Nonomuraea longicatena
- Stabilit?t:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
|
| Alarmwort |
Achtung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H371 |
Kann die Organe sch?digen. |
Spezifische Zielorgan-Toxizit?t |
Kategorie 2 |
Warnung |
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P260, P264, P270, P309+P311, P405,P501 |
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| Sicherheit |
| P202 |
Vor Gebrauch alle Sicherheitshinweise lesen und verstehen. |
| P260 |
Dampf/Aerosol/Nebel nicht einatmen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P270 |
Bei Gebrauch nicht essen, trinken oder rauchen. |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
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K-252A Chemische Eigenschaften,Einsatz,Produktion Methoden
S-S?tze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
K252a is a staurosporine analog isolated from
Nocardiopsis sp. soil fungi that inhibits protein kinase (PK) C, PKA, Ca
2+/calmodulin-
dependent kinase type II, and phosphorylase kinase with IC50 values of 470, 140, 270, and 1.7 nM, respectively. Because it inhibits neurotrophin receptor tyrosine kinases, K252a at 100-500 nM has been used to suppress trophoblast proliferation and increase apoptosis associated with the disruption of mitochondrial functions in cultured choriocarcinoma cells. Recently, K252a has been shown to inhibit PRK1 (IC50 = 3.2 nM in vitro), a PKC-related kinase that phosphorylates histone H3 at threonine 11 and is involved in androgen-dependent gene expression.
Verwenden
K-252a is used to inhibit protein kinases involved in cell signaling processes, including CaM kinase; phosphorylase kinase, serine/threonine kinases, Trk. It is used to inhibit the actions of nerve growth factor (NGF) on PC1 2 cells and to inhibit smooth muscle myosin light chain kinase .
Definition
ChEBI: A organic heterooctacyclic compound that is a potent inhibitor of protein kinase C and is isolated from Nocardiopsis sp K-252a
Biologische Aktivit?t
Non-selective protein kinase inhibitor; analog of staurosporine. Inhibits PKC (IC 50 = 32.9 nM), Ca 2+ /calmodulin-stimulated phosphodiesterases (IC 50 = 1.3-2.9 μ M), MLCK (K i = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).
K-252A Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
K-252A Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 151)Lieferanten
99533-80-9()Verwandte Suche:
- (9-alpha,10-beta,12-alpha)-este
- [9S,(+)]-2,3,9,10,11,12-Hexahydro-10α-hydroxy-9-methyl-1-oxo-9β,12β-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester
- 9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-I)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9alpha,10beta,12alpha)-
- 9,1-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-I)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9-alpha,10-beta,12-alpha)-
- (9α,10β,12α)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-Methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid Methyl ester
- K 252a(SF 2370)
- 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-0-carboxylicacimethyl
- 9,1-epoxy-1h-diindolo(1,2,3-fg:3’,2’,1’-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-1
- antibiotick252a
- antibioticsf2370
- sf2370
- K-252A, NOCARDIOPSIS SP
- (9S,10R,12R)-2,3,9,10,11,12-HEXAHYDRO-10-HYDROXY-9-METHYL-1-OXO-9,12-EPOXY-1H-DIINDOLO[1,2,3-FG:3',2',1'-KL]PYRROLO[3,4-I][1,6]BENZODIAZOCINE-10-CARBOXYLIC ACID METHYL ESTER
- PROTEIN KINASE INHIBITOR K-252A
- PROTEIN KINASE INHIBITOR FROM NORCARDIOP SIS SP.
- (9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1.2.3-fg.3'.2'.1'-kl]pyrrolo[3.4-
- PROTEIN KINASE INHIBITOR K-252A FROM NOCARDIOPSIS SP.)
- K-252A
- 9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9S,10R,12R)-
- J61687 Protein Kinase Inhibitor K252A
- PROTEIN KINASE INHIBITOR
- (5S,6R,8R)-Methyl 6-hydroxy-13-oxo-6,7,8,13,14,15-hexahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate
- K252a, protein and CAM kinase inhibitor
- 99533-80-9
- BioChemical
- Antibiotics
- Antibiotics A to Z
- Antibiotics G-M
- antibiotic
- Protein Kinase InhibitorsEnzymes, Inhibitors, and Substrates
- Antibiotics
- Antibiotics A to
- Kinase/Phosphatase Biology
- Protein Kinases and Phosphatases
- Serine/Threonine Kinase Biology
- Serine/Threonine Kinase Inhibitors
- Protein Kinase
- Antibiotics G-MCell Signaling and Neuroscience
- Protein Kinase Inhibitors and Related ProductsKinase/Phosphatase Biology
