K-252A

ChemicalBook > CAS DataBase List > K-252A

Product Name: K-252A
CAS No.: 99533-80-9
Chemical Name: K-252A
Synonyms: PROTEIN KINASE INHIBITOR;sf2370;K-252A;antibiotick252a;K 252a(SF 2370);antibioticsf2370;K-252A, NOCARDIOPSIS SP;(9-alpha,10-beta,12-alpha)-este;PROTEIN KINASE INHIBITOR K-252A;J61687 Protein Kinase Inhibitor K252A
CBNumber: CB9493885
Molecular Formula: C27H21N3O5
Formula Weight: 467.47
MOL File: 99533-80-9.mol

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K-252A Property

Melting point:: 262-273℃ (decomposition) (methanol )
Boiling point:: 685.3±55.0 °C(Predicted)
Density: 1.68
Flash point:: 87℃
storage temp.: -20°C
solubility: DMF: 1 mg/mL
form: Lyophilized solid.
pka: 11.95±0.40(Predicted)
color: White or off-white
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

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Safety

Hazard Codes: Xi,T
Risk Statements: 61-20/21/22-68/20/21/22
Safety Statements: 22-24/25-45-36/37-53
RIDADR: NA 1993 / PGIII
WGK Germany: 3
RTECS: NZ0550000
F: 8-10
HS Code: 29349990

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H371May cause damage to organs

Precautionary statements

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: K2015
Product name: K-252a
Purity: ReadyMadeSolution,fromNonomuraealongicatena,>98%
Packaging: 200μL
Price: $223
Updated: 2024/03/01

Sigma-Aldrich

Product number: K1639
Product name: K-252a
Purity: fromNonomuraealongicatena,≥98%(HPLC)
Packaging: 100μg
Price: $225
Updated: 2024/03/01

Sigma-Aldrich

Product number: 05288
Product name: K-252a
Purity: from Nocardiopsis sp.
Packaging: 100UG-F
Price: $171
Updated: 2024/03/01

Sigma-Aldrich

Product number: 82497
Product name: K-252a
Purity: from Nocardiopsis sp., ≥96.0% (HPLC)
Packaging: 1mg
Price: $3800
Updated: 2023/01/07

Sigma-Aldrich

Product number: 05288
Product name: K-252a
Purity: fromNocardiopsissp.
Packaging: 100μg
Price: $160
Updated: 2023/01/07

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K-252A Chemical Properties,Usage,Production

Description

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. 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. 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.

Uses

K-252a is used to inhibit protein kinases involved in cell signaling processes, including CaM kinase; phosphorylase kinase, serine/threonine kinases, Trk. It is used to inhibit the actions of nerve growth factor (NGF) on PC1 2 cells and to inhibit smooth muscle myosin light chain kinase .

Definition

ChEBI: A organic heterooctacyclic compound that is a potent inhibitor of protein kinase C and is isolated from Nocardiopsis sp K-252a

Biological Activity

Non-selective protein kinase inhibitor; analog of staurosporine. Inhibits PKC (IC 50 = 32.9 nM), Ca 2+ /calmodulin-stimulated phosphodiesterases (IC 50 = 1.3-2.9 μ M), MLCK (K i = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).

Biochem/physiol Actions

Potent inhibitor of various protein kinases including protein kinase A, C, and G. It is is reported to selectively inhibit the actions of nerve growth factor (NGF) on PC1 2 cells and has been shown to inhibit smooth muscle myosin light chain kinase .

storage

-20°C

References

1) Kase et al. (1987), K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436 2) Hashimoto et al. (1991), Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative KT5926; Biochem. Biophys. Res. Commun., 181 423 3) Berg et al. (1992), K-252a inhibits nerve growth factor-induced trk proto-ooncogene tyrosine phosphorylation and kinase activity; J. Biol. Chem., 267 13 4) Ruegg et al. (1989), Staurosporine, K-252 and UCN-01: potent but non-specific inhibitors of protein kinases; Trends Pharmacol. Sci., 10 218 5) Mohri et al. (1999), K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c; Cancer Invest., 17 391

K-252A Preparation Products And Raw materials

Raw materials

Preparation Products

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K-252A Suppliers

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99533-80-9, K-252ARelated Search:

PROTEIN KINASE INHIBITOR KT 5823 1,3,5,7,9-Pentaoxa-252, 452,652,852-tetraplumbacyclotridec-11 -ene-10,13-dione, (Z)- Amberlite 252, Ion Exchange Resin HC-252 AKOS 213-252 POTASSIUM NITRATE EXTRA PURE, B. P.,FCC, E 252 PROTEIN KINASE INHIBITOR KT 5720 C.I. Acid Red 252 NSC 252 CAMP-DEPENDENT PROTEIN KINASE INHIBITOR,PROTEIN KINASE INHIBITOR, CAMP-DEPENDENT GP120 (252-272) (1) CAMP-DEPENDENT PROTEIN KINASE INHIBITOR (14-24) AMIDE AMBERLITE(R) 252,AMBERLITE(R) 252C protein kinase inhibitor KT 5926 protein kinase inhibitor peptide protein kinase inhibitor peptide (6-24) cGMP-Dependent Protein Kinase Inhibitor Peptide 7-CHLORO-3-(CYCLOPROPYLCARBONYL)-4-HYDROXY-2(1H)-QUINOLINE[L-701, 252]

(9-alpha,10-beta,12-alpha)-este

[9S,(+)]-2,3,9,10,11,12-Hexahydro-10α-hydroxy-9-methyl-1-oxo-9β,12β-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester

9,12-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-I)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9alpha,10beta,12alpha)-

9,1-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-I)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9-alpha,10-beta,12-alpha)-

(9α,10β,12α)-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

K 252a(SF 2370)

2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-0-carboxylicacimethyl

9,1-epoxy-1h-diindolo(1,2,3-fg:3’,2’,1’-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-1

antibiotick252a

antibioticsf2370

sf2370

K-252A, NOCARDIOPSIS SP

K-252A

(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

PROTEIN KINASE INHIBITOR

PROTEIN KINASE INHIBITOR K-252A

PROTEIN KINASE INHIBITOR FROM NORCARDIOP SIS SP.

(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-

PROTEIN KINASE INHIBITOR K-252A FROM NOCARDIOPSIS SP.)

9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9S,10R,12R)-

J61687 Protein Kinase Inhibitor K252A

(5S,6R,8R)-Methyl 6-hydroxy-13-oxo-6,7,8,13,14,15-hexahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate

99533-80-9

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