K-252c

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
K-252c is a cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC) and protein kinase A (PKA) with IC50 value of 2.45 μM and 25.7 μM, respectively. This component was inhibits β-lactamase, malate dehydrogenase and chymotrypsin with IC50 values of 8, 8 and 10 μM respectively [1].
Protein kinase is known as kinase enzymes that modify other proteins by chemically adding phosphate groups to them (phosphorylation). Phosphorylation can result in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins in the cells. PKA and PKC are important family member of AGC kinases.
K-252a was previously shown to block nerve growth factor (NGF)-induced neurite outgrowth and the changes in protein phosphorylation elicited by NGF in PC12h cells [2].
The effect of K-252c was also investigated on the severe combined immunodeficient (SCID) mouse-human skin model of psoriasis. It was shown that psoriasis significantly improved after 2 weeks treatment of K-252c [3].
References:
1. Fabre S, Prudhomme M, Rapp M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem 1993,1:193-196.
2. Hashimoto S. K-252a, a potent protein kinase inhibitor, blocks nerve growth factor-induced neurite outgrowth and changes in the phosphorylation of proteins in PC12h cells. J Cell Biol 1988,107:1531-1539.
3. Raychaudhuri SP, Sanyal M, Weltman H, Kundu-Raychaudhuri S. K252a, a high-affinity nerve growth factor receptor blocker, improves psoriasis: an in vivo study using the severe combined immunodeficient mouse-human skin model. J Invest Dermatol 2004,122:812-819.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 311.34 |
Cas No. | 85753-43-1 |
Formula | C20H13N3O |
Synonyms | Staurosporinone |
Solubility | ≥15.55mg/mL in DMSO |
Chemical Name | 6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one |
SDF | Download SDF |
Canonical SMILES | O=C1C2=C(C3=CC=CC=C3N4)C4=C(NC5=CC=CC=C65)C6=C2CN1 |
Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Description | K-252c is a cell-permeable inhibitor of protein kinase C (PKC) with IC50 value of 2.45 μM. | |||||
Targets | PKC | PKA | ||||
IC50 | 2.45 μM | 25.7 μM |
Quality Control & MSDS
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Chemical structure
