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K2015

Sigma-Aldrich

K-252a

Ready Made Solution, from Nonomuraea longicatena, >98%

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Synonym(s):
SF 2370
Empirical Formula (Hill Notation):
C27H21N3O5
CAS Number:
Molecular Weight:
467.47
EC Number:
MDL number:
PubChem Substance ID:
NACRES:
NA.77

biological source

Nonomuraea longicatena

Quality Level

assay

>98%

form

solution

shipped in

dry ice

storage temp.

−20°C

SMILES string

[H][C@]12C[C@](O)(C(=O)OC)[C@](C)(O1)n3c4ccccc4c5c6CNC(=O)c6c7c8ccccc8n2c7c35

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

InChI key

KOZFSFOOLUUIGY-SOLYNIJKSA-N

Gene Information

human ... NTRK1(4914)
rat ... Prkca(24680)

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1 of 4

This Item
SML2737HPA070395567051-M
K-252a Ready Made Solution, from Nonomuraea longicatena, >98%

K2015

K-252a

AER-271 ≥98% (HPLC)

SML2737

AER-271

Sinefungin InSolution, ≥95%, antibiotic

567051-M

Sinefungin

assay

>98%

assay

≥98% (HPLC)

assay

-

assay

≥95% (HPLC)

Quality Level

200

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

shipped in

dry ice

shipped in

-

shipped in

wet ice

shipped in

-

biological source

Nonomuraea longicatena

biological source

-

biological source

rabbit

biological source

-

Biochem/physiol Actions

K-252a is also a specific inhibitor of Trk (tyrosine kinase) receptors and selectively blocks the effect of nerve growth factor. At lower concentrations, K-252a acts as a neuroprotective compound prompting survival of primary neuronal cultures. K-252a induces cell cycle arrest and apoptosis by inhibiting both Cdc2 and Cdc25c. K-252a improves psoriasis in a SCID mouse-human skin model and also suppresses referred mechanical hypersensitivity and neuropeptide up-regulation associated with acute pancreatitis.

Features and Benefits

This compound is featured on the Met and PKC pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Physical form

Supplied as a 0.2 μm-filtered 1 mM solution in dimethyl sulfoxide (DMSO).

related product

Product No.
Description
Pricing

Storage Class

10 - Combustible liquids

wgk_germany

WGK 1

flash_point_f

188.6 °F - closed cup

flash_point_c

87 °C - closed cup

ppe

Eyeshields, Gloves, multi-purpose combination respirator cartridge (US)


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Z Pawlowska et al.
Journal of neurochemistry, 60(2), 678-686 (1993-02-01)
The phosphorylation of surface proteins by ecto-protein kinase has been proposed to play a role in mechanisms underlying neuronal differentiation and their responsiveness to nerve growth factor (NGF). PC12 clones represent an optimal model for investigating the mode of action
Winston, J.H., et al.
Pain, 4, 329-337 (2003)
L S Chin et al.
Cancer investigation, 17(6), 391-395 (1999-08-06)
The indole carbazole K252a has been shown in previous studies to inhibit the platelet-derived growth factor signal transduction pathway in gliomas. Because K252a has nonspecific effects on protein kinase function, we studied its effect on cyclin-dependent kinases (CDK) and cell
M A Glicksman et al.
Journal of neurochemistry, 64(4), 1502-1512 (1995-04-01)
The organic molecule K-252a promoted cell survival, neurite outgrowth, and increased choline acetyltransferase (ChAT) activity in rat embryonic striatal and basal forebrain cultures in a concentration-dependent manner. A two- to threefold increase in survival was observed at 75 nM K-252a
Haridas B Rode et al.
Bioorganic & medicinal chemistry, 19(1), 429-439 (2010-12-07)
Here we present the synthesis and biological activity of a series of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase (MLCK) and the epidermal growth factor receptor kinase (EGFR). The inhibitory effect of these molecules was found to be dependent

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