A staurosporine analog that inhibits PKC

K252a – 5 mg

Brand:
Cayman
CAS:
99533-80-9
Storage:
-20
UN-No:
Non-Hazardous - /

K252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi that inhibits protein kinase (PK) C, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase with IC50 values of 470, 140, 270, and 1.7 nM, respectively.{21294,17276} Because it inhibits neurotrophin receptor tyrosine kinases, K252a at 100-500 nM has been used to suppress trophoblast proliferation and increase apoptosis associated with the disruption of mitochondrial functions in cultured choriocarcinoma cells.{21290} Recently, K252a has been shown to inhibit PRK1 (IC50 = 3.2 nM in vitro), a PKC-related kinase that phosphorylates histone H3 at threonine 11 and is involved in androgen-dependent gene expression.{21798}  

 

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SKU: 11338 - 5 mg Category:

Description

A staurosporine analog that inhibits PKC, PKA, CaMKII, and phosphorylase kinase (IC50s = 470, 140, 270, and 1.7 nM, respectively); inhibits PRK1 (IC50 = 3.2 nM in vitro), a PKC-related kinase that phosphorylates histone H3 at threonine 11

Formal name: 2,3,9S,10R,11,12R-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, methyl ester

Synonyms:  SF 2370

Molecular weight: 467.5

CAS: 99533-80-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|cAMP Signaling

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