K252b

K252b is a staurosporine analog and PKC inhibitor that suppresses DNA synthesis. It also inhibits microbial ectoprotein kinases and inhibits IgE cross-linking-dependent degranulation in basophils.

Product information

CAS Number: 99570-78-2

Molecular Weight: 453.45

Formula: C26H19N3O5

Chemical Name:  7-hydroxy-8-methyl-15-oxo-5,6,7,8,14,15-hexahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-7-carboxylic acid

Smiles: C[C@]12O[C@H](C[C@]1(O)C(O)=O)N1C3=C4C(=C5CNC(=O)C5=C3C3=CC=CC=C13)C1=CC=CC=C1N24

InChiKey: AMSOPBXQXSAAAC-PLZPTFKGSA-N

InChi: InChI=1S/C26H19N3O5/c1-25-26(33,24(31)32)10-17(34-25)28-15-8-4-2-6-12(15)19-20-14(11-27-23(20)30)18-13-7-3-5-9-16(13)29(25)22(18)21(19)28/h2-9,17,33H,10-11H2,1H3,(H,27,30)(H,31,32)/t17-,25+,26+/m1/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Teshima R, Saito Y, Ikebuchi H, Rajiva De Silva N, Morita Y, Nakanishi M, Sawada J, Kitani S. Effect of an ectokinase inhibitor, K252b, on degranulation and Ca2+ signals of RBL-2H3 cells and human basophils. J Immunol. 1997 Jul 15;159(2):964-9. PubMed PMID: 9218617.
2. Ross AH, McKinnon CA, Daou MC, Ratliff K, Wolf DE. Differential biological effects of K252 kinase inhibitors are related to membrane solubility but not to permeability. J Neurochem. 1995 Dec;65(6):2748-56. PubMed PMID: 7595574.
3. Takeda M, Takahashi M, Hara N, Matsumoto S. Glial cell line-derived neurotrophic factor modulates the excitability of nociceptive trigeminal ganglion neurons via a paracrine mechanism following inflammation. Brain Behav Immun. 2013 Feb;28:100-7. doi: 10.1016/j.bbi.2012.10.023. Epub 2012 Nov 3. PubMed PMID: 23131757.
4. Bacot SM, Feldman GM, Yamada KM, Dhawan S. Pathogenic prion protein fragment (PrP106-126) promotes human immunodeficiency virus type-1 infection in peripheral blood monocyte-derived macrophages. Virology. 2015 Feb;476:372-6. doi: 10.1016/j.virol.2014.11.032. Epub 2015 Jan 9. PubMed PMID: 25589240; PubMed Central PMCID: PMC5282598.
5. Makino K, Kawamura K, Sato W, Kawamura N, Fujimoto T, Terada Y. Inhibition of uterine sarcoma cell growth through suppression of endogenous tyrosine kinase B signaling. PLoS One. 2012;7(7):e41049. doi: 10.1371/journal.pone.0041049. Epub 2012 Jul 23. PubMed PMID: 22911740; PubMed Central PMCID: PMC3402458.

Products are for research use only. Not for human use.