K-252a

BML-EI152

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Protein kinase inhibitor

Alkaloid isolated from soil fungi. General, cell permeable protein kinase inhibitor. Acts by binding to the ATP binding domain of the kinase. Potent inhibitor of Ca²⁺/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC) (K_i=25nM), trk tyrosine kinase family members (gp140trk; IC₅₀ =3nM) and cGMP-dependent protein kinase (PKG). Binds with high affinity to neuroblastoma membrane (2.7nM), promoting survival of primary neuronal cultures (75nM) and induction of neurite outgrowth in SH-SY5Y neuroblastoma cells along with phosphorylation of pp125 focal adhesion protein tyrosine kinase. Induces apoptosis.

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Product Details

Appearance	Lyophilized solid.
CAS	99533-80-9
Couple Target	CaM kinase, MLCK, PKA, PKC, PKG, Trk
Couple Type	Inhibitor
Formula	C₂₇H₂₁N₃O₅
MW	467.5
Purity	≥98% (HPLC)
RTECS	NZ0550000
Solubility	Soluble in DMSO (1mg/ml) or dimethyl formamide (1mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C.
Handling	Protect from light.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Mountain-cultivated ginseng protects against cognitive impairments in aged GPx-1 knockout mice via activation of Nrf2/ChAT/ERK signaling pathway: B.T. Nguyen, et al.; J. Ginseng Res. 47, 561 (2023), Abstract
Development of actionable targets of multi-kinase inhibitors (AToMI) screening platform to dissect kinase targets of staurosporines in glioblastoma cells: O.V. Denisova, et al.; Sci. Rep. 12, 13796 (2022), Abstract
Involvement of Rac1 in macrophage activation by brain-derived neurotrophic factor: S. Sasaki, et al.; Mol. Biol. Rep. 48, 5249 (2021), Abstract
Trimeprazine increases IRS2 in human islets and promotes pancreatic β cell growth and function in mice: Kuznetsova, A., Yu, Y., et al.; JCI Insight 1, (2016), Abstract
Self-amplified BDNF transcription is a regulatory system for synaptic maturation in cultured cortical neurons: S. Nakajima, et al.; Neurochem. Int. 91, 55 (2015), Application(s): Cell culture , Abstract
Luteolin induces microRNA-132 expression and modulates neurite outgrowth in PC12 cells: Lin, L. F., Chiu, S. P., et al.; PLoS One 7, e43304 (2012), Abstract
Neurotrophic effect of citrus 5-hydroxy-3,6,7,8,3′,4′-hexamethoxyflavone: promotion of neurite outgrowth via cAMP/PKA/CREB pathway in PC12 cells: Lai, H. C., Wu, M. J., et al.; PLoS One 6, e28280 (2011), Abstract
A conserved cysteine motif is critical for rice ceramide kinase activity and function: Bi, F. C., Zhang, Q. F., et al.; PLoS One 6, e18079 (2011), Abstract
Nerve growth factor and substance P regulation in nasal sensory neurons after toluene diisocyanate exposure: Wilfong, E. R., Dey, R. D., et al.; Am. J. Respir. Cell Mol. Biol. 30, 793 (2004), Abstract
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review, Abstract

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K-252a

BML-EI152

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Handling & Storage

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