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MW 466.5 Da, Purity >98%. Potent, cell-permeable, broad spectrum inhibitor of protein kinases. Kinases inhibited include: protein kinase C (IC50 = 3 nM), cAMP-dependent protein kinase (IC50 = 8 nM) and p60v-src (IC50 = 6 nM).

Also available as a solid (ab120056).

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Key facts

CAS number

62996-74-1

Purity

> 98%

Form

Solid

Molecular weight

466.5 Da

Molecular formula

C28H26N4O3

PubChem identifier

44259

Nature

Synthetic

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Alternative names

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MW 466.5 Da, Purity >98%. Potent, cell-permeable, broad spectrum inhibitor of protein kinases. Kinases inhibited include: protein kinase C (IC50 = 3 nM), cAMP-dependent protein kinase (IC50 = 8 nM) and p60v-src (IC50 = 6 nM).

Also available as a solid (ab120056).

Alternative names

Key facts

Purity

> 98%

PubChem identifier

44259

Biochemical name

Staurosporine

Biological description

Potent, cell-permeable, broad spectrum inhibitor of protein kinases. Kinases inhibited include: protein kinase C (IC50 = 3 nM), cAMP-dependent protein kinase (IC50 = 8 nM) and p60v-src (IC50 = 6 nM).

Also available as a solid (ab120056).

Canonical SMILES

CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC

Isomeric SMILES

C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC

InChI

InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1

InChIKey

HKSZLNNOFSGOKW-FYTWVXJKSA-N

IUPAC name

(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one

Storage

Shipped at conditions

Ambient - Can Ship with Ice

Appropriate long-term storage conditions

+4°C

Storage information

Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary info

Biological function summary

PKC isoforms regulate cellular functions like proliferation differentiation and apoptosis. These proteins are part of larger signaling complexes participating in dynamic equilibrium states that determine cellular fate. For example PKC epsilon often interacts within complexes modulating oncogenic pathways while PKC beta 2 plays roles in immune response modulation. The distinct expression patterns and interactions of these isoforms enable them to assume specific biological roles in different tissues.

Activity summary

Protein kinase C (PKC) is a family of serine/threonine kinases essential in cellular signaling. The PKC family includes several isoforms such as PKC delta PKC epsilon PKC beta 2 PKC gamma and PKC theta (also known as PRKCQ). These proteins exhibit diverse molecular masses ranging from about 78 kDa to 82 kDa. PKCs are broadly expressed in various tissues and cells particularly in the brain heart and immune cells. PKC isoforms play significant mechanical roles by phosphorylating various substrate proteins influencing various cellular processes.

Pathways

Several PKC isoforms engage critical cell signaling pathways such as the MAPK/ERK pathway and the PI3K/AKT pathway. In these pathways PKCs modulate various downstream effectors coordinating signals that influence gene expression and cell survival. PKC delta has significant associations with the MAPK cascade while PKC theta interacts closely with PI3K. These interactions are necessary for linking external signals to intracellular responses thereby acting as converging points for signaling pathways impacting multiple cellular functions.

Associated diseases and disorders

PKC isoforms associate with cancer and cardiovascular diseases. PKC epsilon often links with cancer progression particularly breast and lung cancers by interacting with oncogenes that promote tumor growth. PKC beta 2 shows connections with metabolic disorders especially in the context of cardiac dysfunction. Disease links may involve other proteins such as Src kinase which interacts with PKC pathways affecting cell motility and survival in cancerous conditions. Understanding these relationships aids in developing therapeutic strategies targeting PKC-related pathways in disease treatment.

Product promise

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6 product images

  • Chemical Structure - Staurosporine, Protein kinase inhibitor (ab120056), expandable thumbnail

    Chemical Structure - Staurosporine, Protein kinase inhibitor (ab120056)

    2D chemical structure image of ab120056, Staurosporine, Protein kinase inhibitor

  • Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056), expandable thumbnail

    Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056)

    HeLa and Jurkat cells were treated with 1 µM Staurosporine (STS) (ab120056) for 4 hours in complete cell culture media to induce apoptosis and cleaved PARP protein. Untreated and STS treated HeLa and Jurkat lysates were prepared in 1X Cell Extraction Buffer PTR and tested the Cleaved PARP SimpleStepTM ELISA. Raw OD 450 nm values are shown for 500 µg/mL lysate loads.

  • Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056), expandable thumbnail

    Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056)

    Lane 1: HeLa, vehicle (DMSO) treated for 4 hours Lane 2: HeLa 1 μM staurpsorine (ab120056), 4 hours Load 20 μg/lane 5% milk/PBST for block and antibody diluent Primary antibodies (2 hours, room temp) All lanes: ab136812 250X Primary Antibodies Cocktail, 1/250 dilution Secondary antibodies (1 hour, room temp) All lanes: ab136812 100X HRP-Conjugated Secondary Antibodies Cocktail, 1/100 dilution

  • Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056), expandable thumbnail

    Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056)

    Example of HeLa staurosporine (ab120056) treated cell lysate titration. Background-subtracted data values (mean +/- SD) are graphed.

  • Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056), expandable thumbnail

    Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056)

    Example of IC50 determination. HeLa cells were treated with a dose titration of Staurosporine for 4 hours in complete media. Cells were cultured and treated in a 96-well cell culture microtiter plate. Lysates were prepared by direct in-well lysis without media removal: 2X Cell Extraction Buffer PTR was added to an equal volume of media and then resulting lysate was used directly in the Cleaved PARP SimpleStepTM ELISA assay. Raw values for triplicate measurements are plotted. The calculated IC50 is 0.77 μM.

  • Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056), expandable thumbnail

    Functional Studies - Staurosporine, Protein kinase inhibitor (ab120056)

    Demonstration of Cleaved PARP capture antibody specificity by western blot assay. 20 μg of HeLa extracts that were untreated or treated for 4 hours with 1 μM Staurosporine were analyzed by western blot. The GAPDH blot is included to show the relative loads of each lysate. In the HeLa cell line, Staurosporine treatment is required to detect cleaved PARP protein, as observed in the SimpleStep ELISA.

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