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K-252A

K-252A Structure
K-252A structure
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
Molecular Weight:
467.47
MDL Number:
MFCD09878276
MOL File:
99533-80-9.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59
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K-252A Properties

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
pka 11.95±0.40(Predicted)
form Lyophilized solid.
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.
NCI Dictionary of Cancer Terms protein kinase inhibitor
FDA UNII IV7H45AM5B

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS08
Signal word  Danger
Hazard statements  H360D-H371
Precautionary statements  P202-P260-P264-P270-P280-P308+P311
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
NFPA 704
0
2 0

K-252A price More Price(15)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich K2015 K-252a ReadyMadeSolution,fromNonomuraealongicatena,>98% 99533-80-9 200μL $223 2024-03-01 Buy
Sigma-Aldrich K1639 K-252a fromNonomuraealongicatena,≥98%(HPLC) 99533-80-9 100μg $225 2024-03-01 Buy
Sigma-Aldrich 05288 K-252a from Nocardiopsis sp. 99533-80-9 100UG-F $171 2024-03-01 Buy
Sigma-Aldrich 82497 K-252a from Nocardiopsis sp., ≥96.0% (HPLC) 99533-80-9 1mg $3800 2023-01-07 Buy
Sigma-Aldrich 05288 K-252a fromNocardiopsissp. 99533-80-9 100μg $160 2023-01-07 Buy
Product number Packaging Price Buy
K2015 200μL $223 Buy
K1639 100μg $225 Buy
05288 100UG-F $171 Buy
82497 1mg $3800 Buy
05288 100μg $160 Buy

K-252A Chemical Properties,Uses,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

KT5823

K-252A Suppliers

Global( 143)Suppliers
Supplier Tel Email Country ProdList Advantage
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
TopScience Biochemical 		00852-68527855 info@itopbiochem.com China Hong Kong 902 58
Fuxin Pharmaceutical 		+86-021-021-50872116 +8613122107989 contact@fuxinpharm.com China 10297 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
Alfa Chemistry 		+1-5166625404 Info@alfa-chemistry.com United States 21317 58
Wuhan Topule Biopharmaceutical Co., Ltd 		+8618327326525 masar@topule.com China 8474 58
Jilin Chinese Academy of Sciences-yanshen Technology 		+undefined18143011203 info@chemextension.com China 42057 58
Aladdin Scientific 		+1-833-552-7181 sales@aladdinsci.com United States 57511 58
3B Pharmachem (Wuhan) International Co.,Ltd. 821-50328103-801 18930552037 3bsc@sina.com China 15848 69
Chemsky (shanghai) International Co.,Ltd 021-50135380 shchemsky@sina.com China 15421 60
Supplier Advantage
BOC Sciences 		58
TopScience Biochemical 		58
Fuxin Pharmaceutical 		58
TargetMol Chemicals Inc. 		58
Alfa Chemistry 		58
Wuhan Topule Biopharmaceutical Co., Ltd 		58
Jilin Chinese Academy of Sciences-yanshen Technology 		58
Aladdin Scientific 		58
3B Pharmachem (Wuhan) International Co.,Ltd. 69
Chemsky (shanghai) International Co.,Ltd 60

99533-80-9(K-252A)Related 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]

1of4

(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 (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 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.) K-252A 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 PROTEIN KINASE INHIBITOR (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