Product overview

Name K-252a
Alternative names SF 2370
Purity >97%
Description Non-selective protein kinase inhibitor
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Biological Data

Biological description Non-selective protein kinase inhibitor (IC50 values are 10-30 nM for serine/threonine protein kinases). PKC and Ca2+ / calmodulin-stimulated phosphodiesterase inhibitor (IC50 values are 32.9 nM and 1.8 - 2.8 µM respectively). Competitively inhibits myosin light chain kinase (MLCK) - may interact with the ATP-binding domain (Ki = 20 nM). Blocks neuronal differentiation by potently inhibiting NGF receptor gp140trk tyrosine protein kinase (IC50 = 3nM). Cell permeable and shows potential anti-tumor actions.

Solubility & Handling

Solubility overview Soluble in DMSO (1mg/ml) or DMF (1mg/ml)
Storage instructions -20°C
Storage of solutions Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Chemical Data

Purity >97%
Chemical name (9S,10R,12R)-2,3,9,10,11,12-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
Molecular Weight 467.5
Chemical structure K-252a  [99533-80-9] Chemical Structure
Molecular Formula C27H21N3O5
CAS Number 99533-80-9
PubChem identifier 3035817
SMILES C[C@@]12[C@](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)(C(=O)OC)O
Source Nocardiopsis sp
InChi InChI=1S/C27H21N3O5/c1-26-27(33,25(32)34-2)11-18(35-26)29-16-9-5-3-7-13(16)20-21-15(12-28-24(21)31)19-14-8-4-6-10-17(14)30(26)23(19)22(20)29/h3-10,18,33H,11-12H2,1-2H3,(H,28,31)/t18-,26+,27+/m1/s1
InChiKey KOZFSFOOLUUIGY-SOLYNIJKSA-N
MDL number MFCD00161522

References for K-252a

References are publications that support the biological activity of the product
  • K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors.

    Tapley P et al (1992) Oncogene 7(2) : 371-81.
  • K-252a, a novel microbial product, inhibits smooth muscle myosin light chain kinase.

    Nakanishi S et al (1988) J Biol Chem 263(13) : 6215-9.
  • The effect of K-252a, a potent microbial inhibitor of protein kinase, on activated cyclic nucleotide phosphodiesterase.

    Matsuda Y et al (1988) Biochem J 256(1) : 75-80.
  • K-252a, a potent inhibitor of protein kinase C from microbial origin.

    Kase H et al (1986) J Antibiot (Tokyo) 39(8) : 1059-65.

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