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.
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- No. CAS: 85753-43-1
- Fòrmula: C20H13N3O
- Peso molecular:311.34
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Help & FAQs
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Actividad biológica
IC50: 2.45 µM (PKC)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16 | IC50 |
4.8 μM
Compound: 11
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Antiproliferative activity against B16 mouse melanoma cells
Antiproliferative activity against B16 mouse melanoma cells
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[PMID: 8893841] |
| HCT-116 | IC50 |
1.72 μM
Compound: 3 (K-252c)
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In vitro antiproliferative activity against HCT116 ( human colon) cell line.
In vitro antiproliferative activity against HCT116 ( human colon) cell line.
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[PMID: 14552792] |
| HCT-116 | IC50 |
1.72 μM
Compound: 9
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Inhibition of human HCT(colon) carcinoma cell proliferation
Inhibition of human HCT(colon) carcinoma cell proliferation
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[PMID: 14552791] |
| HCT-116 | IC50 |
1.72 μM
Compound: K252c
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Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
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[PMID: 27255178] |
| K562 | IC50 |
7.8 μM
Compound: K252c
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Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
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[PMID: 27255178] |
| NCI-H460 | IC50 |
3.2 μM
Compound: 3 (K-252c)
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In vitro antiproliferative activity against NCI-460 (human lung) cell line.
In vitro antiproliferative activity against NCI-460 (human lung) cell line.
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[PMID: 14552792] |
| NCI-H460 | IC50 |
3.2 μM
Compound: 9
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Inhibition of human NCI-H460 (lung) carcinoma cell proliferation
Inhibition of human NCI-H460 (lung) carcinoma cell proliferation
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[PMID: 14552791] |
| P388 | IC50 |
4 μM
Compound: 11
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Antiproliferative activity against P388 Murine Leukemia cells
Antiproliferative activity against P388 Murine Leukemia cells
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[PMID: 8893841] |
| PANC-1 | IC50 |
1.8 μM
Compound: 131
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Inhibition of Gli1-mediated transcription expressed in human PANC1 cells
Inhibition of Gli1-mediated transcription expressed in human PANC1 cells
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[PMID: 19309080] |
| PANC-1 | IC50 |
2.7 μM
Compound: 131
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Inhibition of Gli2-mediated transcription expressed in human PANC1 cells
Inhibition of Gli2-mediated transcription expressed in human PANC1 cells
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[PMID: 19309080] |
| Sf21 | IC50 |
61 nM
Compound: 23, K-252c
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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
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[PMID: 19427203] |
Chemical Information
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No. CAS 85753-43-1
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Appearance Solid
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Peso molecular 311.34
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Fòrmula C20H13N3O
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Color White to off-white
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SMILES
O=C1NCC2=C1C3=C(C4=C2C5=C(N4)C=CC=C5)NC6=C3C=CC=C6
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Structure Classification
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Initial Source
Nocardiopsis sp.
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
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Ficha de datos (276 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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