K-252c
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.02%
- CAS No.: 85753-43-1
- Formula: C20H13N3O
- Molecular Weight:311.34
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Storage:
-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]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
IC50: 2.45 µM (PKC)[1].
Cellular Effect
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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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CAS No. 85753-43-1
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Appearance Solid
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Molecular Weight 311.34
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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)
K-252c Related Classifications
HY-N6736 Related Classifications
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