PP1

BML-EI275

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Src kinase inhibitor

A highly potent and selective inhibitor of Src family tyrosine kinases, IC₅₀=5 nM for p56^lck; p59^fynT=6 nM; p60^src=170 nM. Inhibition of Src family kinases by PP1 has been shown to: prevent a-thrombin-stimulated Akt phosphorylation, delay PAF-mediated STAT3 phosphorylation, block Zn²⁺-induced Ras activation, block adhesion-dependent tyrosine phosphorylation of p105^{HEF1 5}, and inhibit HLA-DR-induced tyrosine phosphorylation without affecting the activation of ERK1/2.

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Product Details

Appearance	Tan solid.
CAS	172889-26-8
Couple Target	Src kinase
Couple Type	Inhibitor
Formula	C₁₆H₁₉N₅
MW	281.4
Purity	≥98% (TLC)
Solubility	Soluble in DMSO (25mg/ml), slightly soluble in 100% ethanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Novel inhibitors of microtubule organization and phragmoplast formation in diverse plant species: Y. Kimata, et al.; Life Sci. Alliance 6, e202201657 (2023), Abstract
Gαs proteins Activate p72 Syk and p60-c-Src Tyrosine Kinases to Mediate Sickle Red Blood Cell Adhesion to Endothelium via LW-αvβ3 and CD44-CD44 Interactions: E. Chiou, et al.; Int. J. Biochem. Cell. Biol. 65, 40 (2015), Application(s): Cell Culture, Abstract
α6 integrin transactivates insulin-like growth factor receptor-1 (IGF-1R) to regulate caspase-3-mediated lens epithelial cell differentiation initiation: S. Basu, et al.; J. Biol. Chem. 289, 3842 (2014), Abstract
Regulation of hERG and hEAG channels by Src and by SHP-1 tyrosine phosphatase via an ITIM region in the cyclic nucleotide binding domain: Schlichter, L. C., Jiang, J., et al.; PLoS One 9, e90024 (2014), Abstract
Distinct roles for N-Cadherin linked c-Src and fyn kinases in lens development: Leonard, M., Zhang, L., et al.; Dev. Dyn. 242, 469 (2013), Abstract
A novel mechanism of sustained platelet αIIbβ3 activation via PEAR1: Kauskot, A., Di Michele, M., et al.; Blood 119, 4056 (2012), Abstract
Phosphorylation and transport in the Na-K-2Cl cotransporters, NKCC1 and NKCC2A, compared in HEK-293 cells: Hannemann, A., Flatman, P. W., et al.; PLoS One 6, e17992 (2011), Abstract
EGF receptor exposed to oxidative stress acquires abnormal phosphorylation and aberrant activated conformation that impairs canonical dimerization: Filosto, S., Khan, E. M., et al.; PLoS One 6, e23240 (2011), Abstract
Collagen type I selectively activates ectodomain shedding of the discoidin domain receptor 1: involvement of Src tyrosine kinase: Slack, B. E., Siniaia, M. S., et al.; J. Cell. Biochem. 98, 672 (2006), Abstract
Prolactin induces c-Myc expression and cell survival through activation of Src/Akt pathway in lymphoid cells: Domínguez-Cáceres, M. A., García-Martínez, J. M., et al.; Oncogene 23, 7378 (2004), Abstract

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PP1

BML-EI275

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