K252c free base

K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor.

For research use only. Not for human or veterinary use.

Target Beta-lactamase PKC Bacterial Apoptosis

Research area Infection Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

K252c structure

CAS No.: 85753-43-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 898.00	BP-02394-25mg	In stock	Get quote
50 mg	USD 1,798.00	BP-02394-50mg	In stock	Get quote
100 mg	USD 3,098.00	BP-02394-100mg	In stock	Get quote
250 mg	Inquire	BP-02394-250mg	In stock	Inquire

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Description

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.

Biological activity

K-252c is a inhibitor of protein kinase C (IC50 = 2.45 μM) that displays ~ 10-fold selectivity over protein kinase A (IC50 = 25.7 μM). Also inhibits β-lactamase, malate dehydrogenase and chymotrypsin (IC50 values are 8, 8 and 10 μM respectively). Exhibits antiviral activity against GCV-sensitive and -resistant strains of human cytomegalovirus (HCMV) (IC50 values range from 0.13 - 0.32 μM). Shows no activity against herpes simplex virus (HSV).

Identifiers

SMILES: C1C2=C3C4=CC=CC=C4NC3=C5C(=C2C(=O)N1)C6=CC=CC=C6N5
InChIKey: MEXUTNIFSHFQRG-UHFFFAOYSA-N

Specifications

MW (average): 311.3367
Formula: C₂₀H₁₃N₃O
CAS No.: 85753-43-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, sealed storage, away from moisture; In solvent -20°C, 1 month.

Solubility

soluble in DMSO

In vitro: DMSO 7.78 mg/mL

Documents

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).

[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).

[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).

[4]. McGovern, S.L., et al. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003).

Same target

Search Beta-lactamase

Same research area

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