K-252c
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 85753-43-1
- Formel: C20H13N3O
- Molecular Weight:311.34
-
Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle Beta-lactamase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
IC50: 2.45 µM (PKC)[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| B16 | IC50 |
4.8 μM
Compound: 11
|
Antiproliferative activity against B16 mouse melanoma cells
Antiproliferative activity against B16 mouse melanoma cells
|
[PMID: 8893841] |
| HCT-116 | IC50 |
1.72 μM
Compound: 3 (K-252c)
|
In vitro antiproliferative activity against HCT116 ( human colon) cell line.
In vitro antiproliferative activity against HCT116 ( human colon) cell line.
|
[PMID: 14552792] |
| HCT-116 | IC50 |
1.72 μM
Compound: 9
|
Inhibition of human HCT(colon) carcinoma cell proliferation
Inhibition of human HCT(colon) carcinoma cell proliferation
|
[PMID: 14552791] |
| HCT-116 | IC50 |
1.72 μM
Compound: K252c
|
Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
|
[PMID: 27255178] |
| K562 | IC50 |
7.8 μM
Compound: K252c
|
Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
|
[PMID: 27255178] |
| NCI-H460 | IC50 |
3.2 μM
Compound: 3 (K-252c)
|
In vitro antiproliferative activity against NCI-460 (human lung) cell line.
In vitro antiproliferative activity against NCI-460 (human lung) cell line.
|
[PMID: 14552792] |
| NCI-H460 | IC50 |
3.2 μM
Compound: 9
|
Inhibition of human NCI-H460 (lung) carcinoma cell proliferation
Inhibition of human NCI-H460 (lung) carcinoma cell proliferation
|
[PMID: 14552791] |
| P388 | IC50 |
4 μM
Compound: 11
|
Antiproliferative activity against P388 Murine Leukemia cells
Antiproliferative activity against P388 Murine Leukemia cells
|
[PMID: 8893841] |
| PANC-1 | IC50 |
1.8 μM
Compound: 131
|
Inhibition of Gli1-mediated transcription expressed in human PANC1 cells
Inhibition of Gli1-mediated transcription expressed in human PANC1 cells
|
[PMID: 19309080] |
| PANC-1 | IC50 |
2.7 μM
Compound: 131
|
Inhibition of Gli2-mediated transcription expressed in human PANC1 cells
Inhibition of Gli2-mediated transcription expressed in human PANC1 cells
|
[PMID: 19309080] |
| Sf21 | IC50 |
61 nM
Compound: 23, K-252c
|
Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation
Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation
|
[PMID: 19427203] |
Chemical Information
-
CAS. Nr. 85753-43-1
-
Appearance Solid
-
Molecular Weight 311.34
-
Formel C20H13N3O
-
Color White to off-white
-
SMILES
O=C1NCC2=C1C3=C(C4=C2C5=C(N4)C=CC=C5)NC6=C3C=CC=C6
-
Structure Classification
-
Initial Source
Nocardiopsis sp.
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reinheit & Dokumentation
-
Data Sheet (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Pereira, E.R., et al. Structure-activity relationships in a series of substituted indolocarbazoles: Topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties J. Med. Chem. 39(22), 4471-4477 (1996). [Content Brief]
[2]. Liu, R., et al. Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z2039-2 Arch. Pharm. Res. 30(3), 270-274 (2007). [Content Brief]
[3]. Zimmermann, A., et al. Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase Antiviral Res. 48(1), 49-60 (2000). [Content Brief]
[4]. McGovern, S.L., et al. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003). [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
K-252c Related Classifications
HY-N6736 Related Classifications
Powered by Bioz