ChemicalBook > CAS DataBase List > K-252A

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

China 105 China Hong Kong 1 Germany 4 India 1 Japan 3 Switzerland 2 United Kingdom 5 United States 22 Global 143
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15839
Advantage
69
Chemsky (shanghai) International Co.,Ltd
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
15402
Advantage
60
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Fax
021-50323701
Email
market@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4428
Advantage
55
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
ChemStrong Scientific Co.,Ltd
Tel
0755-0755-66853366 13670046396
Fax
0755-28363542
Email
sales@chem-strong.com
Country
China
ProdList
18042
Advantage
56
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51456
Advantage
80
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9806
Advantage
58

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
  • BioChemical
  • Antibiotics
  • Antibiotics A to Z
  • Antibiotics G-M
  • antibiotic
  • Protein Kinase InhibitorsEnzymes, Inhibitors, and Substrates
  • Antibiotics
  • Antibiotics A to
  • Kinase/Phosphatase Biology
  • Protein Kinases and Phosphatases
  • Serine/Threonine Kinase Biology
  • Serine/Threonine Kinase Inhibitors
  • Protein Kinase
  • Antibiotics G-MCell Signaling and Neuroscience
  • Protein Kinase Inhibitors and Related ProductsKinase/Phosphatase Biology