K-252c

Cat. No.: HY-N6736: Data Sheet
COA

SDS
Handling Instructions
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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.

K-252c Chemical Structure

CAS No. : 85753-43-1

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This product is a controlled substance and not for sale in your territory.

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•Related Small Molecules:

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Metallo-β-lactamase (MBL) Serine β-lactamase (SBL)

View All PKC Isoform Specific Products:

View All Isoforms

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 2.45 µM (PKC)^[1].

Cellular Effect

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]

Molecular Weight

311.34

Formula

C₂₀H₁₃N₃O

CAS No.

85753-43-1

Appearance

Solid

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

Microorganisms

Nocardiopsis sp.

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: ≥99.0%

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Data Sheet (276 KB) SDS (251 KB)

COA (258 KB)

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]

K-252c Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K-252c85753-43-1Beta-lactamasePKCBacterialApoptosisβ-lactamaseProtein kinase CInhibitorinhibitorinhibit

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