99570-78-2

Basic information

• Product Name: K-252B
• Synonyms: PROTEIN KINASE INHIBITOR K-252B;K-252B;K-252B, NOCARDIOPSIS SP;K-252B, NOCARDIOPSIS SPECIES;K252B READY MADE;k-252b solution;(9R,10S,12S)-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;Antibiotic K 252b
• CAS NO: 99570-78-2
• Molecular Formula: C26H19N3O5
• Molecular Weight: 453.452
• EINECS: 999-999-2
• Product Categories: Antibiotics G-MSerine/Threonine Kinase Biology;Antibiotics;Antibiotics A to;Protein Kinase C (PKC);Serine/Threonine Kinase Inhibitors;Protein Kinase;antibiotic
• Mol File: 99570-78-2.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 769.8±60.0 °C(Predicted)
• Appearance: /ready-to-use solution
• 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).
• PKA: 3.33±0.40(Predicted)
• 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.
• CAS DataBase Reference: K-252B(CAS DataBase Reference)
• NIST Chemistry Reference: K-252B(99570-78-2)
• EPA Substance Registry System: K-252B(99570-78-2)

Safety Data

• Hazard Codes: Xi
• RIDADR: UN 1993 / PGIII
• Hazardous Substances Data: 99570-78-2(Hazardous Substances Data)

Usage

Description

K-252B is an indolocarbazole compound isolated from the actinomycete Nocardiopsis, which was initially identified as an inhibitor of protein kinase C. However, due to its limited ability to cross the cell membrane, it is primarily used to inhibit extracellular kinases (ectokinases) in cultured cells. K-252B is also known for its inhibitory effects on receptor-mediated degranulation from basophil-like RBL-2H3 cells and human basophils. It is often compared with the closely related, cell-permeable inhibitor K-252A, particularly in studies related to neuronal differentiation.

Uses

Used in Pharmaceutical Industry:
K-252B is used as a potent inhibitor of protein kinase C, Ca2+/calmodulin kinase II, myosin light chain kinase, cAMP-dependent protein kinase (PKA), and cGMP-dependent protein kinase (PKG) for various research and therapeutic applications.
Used in Neurobiology Research:
K-252B is used as an extracellular inhibitor to study the effects of receptor-mediated degranulation from basophil-like RBL-2H3 cells and human basophils, as well as its role in neuronal differentiation.
Used in Neuroprotection:
K-252B is used as a protein tyrosine kinase inhibitor to inhibit the trophic activity of brain-derived neurotrophic factor on dopaminergic (DAergic) neurons and nerve growth factor on basal forebrain cholinergic neurons, potentially contributing to neuroprotection in various conditions.

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

Upstream product

• 99533-80-9 K-252a 
• 244128-10-7 C₄₅H₃₇N₃O₈ 
• 244128-14-1 C₃₃H₂₇N₃O₄Se 
• 244128-13-0 C₃₁H₂₅N₃O₃Se 
• 244128-16-3 C₂₇H₂₀IN₃O₄ 
• 244128-18-5 C₂₈H₂₀N₄O₄ 
• 244128-17-4 C₂₇H₂₁N₃O₄ 
• 244128-15-2 C₂₇H₂₁N₃O₄ 
• 236113-24-9 C₂₅H₂₁N₃O₄ 
• 244128-11-8 C₂₅H₂₀IN₃O₃ 
• 229976-29-8 C₂₅H₁₉N₃O₃ 
• 111359-05-8 C₂₅H₁₇N₃O₃ 

Downstream Products

• 99533-80-9 K-252a 

Relevant articles and documents

FORMULATIONS FOR DERMAL DELIVERY OF POLYMER CONJUGATES OF INDOLOCARBAZOLE COMPOUNDS WITH REDUCED EXPOSURE

Topical formulations to treat skin conditions, such as atopic dermatitis, psoriasis, pruritus, are provided in which a polymer conjugate of an indolocarbazole exhibits reduced systemic exposure. An example formulation includes the TrkA/JAK/MAP kinase antagonist, SNA-125, in a cream formulation.