K-252B Chemical Properties

Boiling point:

769.8±60.0 °C(Predicted)

Density 

1.78±0.1 g/cm3(Predicted)

storage temp. 

−20°C

solubility 

Soluble in DMSO (up to 1 mg/ml) or in DMF (up to 1 mg/ml).

form 

ready-to-use solution

pka

3.33±0.40(Predicted)

color 

White or off-white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months.

Safety Information

Hazard Codes 

Xi

RIDADR 

UN 1993 / PGIII

HS Code 

29349990

MSDS

• Language:English Provider:SigmaAldrich

K-252B Usage And Synthesis

Description

K252b is an indolocarbazole isolated from the actinomycete Nocardiopsis, first described as an inhibitor of protein kinase C. However, as this compound does not freely pass through the cell membrane, it is used to inhibit extracellular kinases (ectokinases) of cells in culture. K252b inhibits receptor-mediated degranulation from basophil-like RBL-2H3 cells (IC₅₀ = 0.5 μg/ml) and human basophils. This extracellular inhibitor is also used in comparison studies with the closely related, cell-permeable inhibitor K252a, particularly in studies of neuronal differentiation.

Chemical Properties

Yellow solid

Uses

K 252b, is an antibiotics, and a known protein tyrosine kinase inhibitor. It has been also shown to inhibit the trophic activity of brain-derived neurotrophic factor on dopaminergic (DAergic) neurons and nerve growth factor on basal forebrain cholinergic neurons.

Uses

K252A is a staurosporine analogue isolated from a Nocardiopsis strain as a potent inhibitor of protein kinase C. K252A exhibits potent antitumour activity but shows no antimicrobial activity in vitro, or in vivo toxicity in rodents. While K252A is a potent inhibitor of Ca2+/calmodulin kinase II, it is also active against other kinases, notably myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and cGMP-dependent protein kinase (PKG).

References

1) Kase et al. (1987), K252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436 2) Makino et al. (2012), Inhibition of uterine sarcoma cell growth through suppression of endogenous tyrosine kinase B signaling; PLoS One, 7 e41049

K-252B(99570-78-2)Related Product Information

• AKOS 213-252
• Amberlite 252, Ion Exchange Resin
• HC-252
• 9-CARBAZOLEPROPIONIC ACID
• KT5720
• 1-(1-METHYL-1H-INDOL-4-YL)METHYLAMINE 97
• 9-ISOPROPYLCARBAZOLE
• 1,3,5,7,9-Pentaoxa-252, 452,652,852-tetraplumbacyclotridec-11 -ene-10,13-dione, (Z)-
• POTASSIUM NITRATE EXTRA PURE, B. P.,FCC, E 252
• C.I. Acid Red 252
• NSC 252
• PROTEIN KINASE INHIBITOR K-252A FROM NOCARDIOPSIS SP.)
• K-252C
• K-252B
• CARBAZOL-9-YL-METHANOL
• 11,12-Dihydroindolo[2,3-a]carbazole
• Hydrochlorofluorocarbon-252 (HCFC-252)
• GP120 (252-272) (1)