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About This Item
Empirical Formula (Hill Notation):
C19H19N5
CAS Number:
Molecular Weight:
317.39
UNSPSC Code:
12352202
Assay
≥99% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
InChI
1S/C19H19N5/c1-19(2,3)24-18-15(17(20)21-11-22-18)16(23-24)14-10-6-8-12-7-4-5-9-13(12)14/h4-11H,1-3H3,(H2,20,21,22)
InChI key
XSHQBIXMLULFEV-UHFFFAOYSA-N
General description
A potent, reversible, ATP-competitive, and cell-permeable inhibitor of Src-family tyrosine kinases that is >800 times more selective for the I338G mutant v-Src (IC50 = 1.5 nM) compared to wild-type v-Src (IC50 = 1.0 µM). Also inhibits wild-type Fyn (IC50 = 600 nM). Also available in InSolution format (Cat. No. 529605).
A potent, reversible, ATP-competitive, cell-permeable and selective inhibitor of Src-family tyrosine kinases that is >800 times more selective for the I338G mutant v-Src (IC50 = 1.5 nM) compared to wild-type v-Src (IC50 = 1 µM). Also inhibits wild-type Fyn (IC50 = 600 nM). Also available in InSolution format (Cat. No. 529605).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
I338G mutant v-Src
I338G mutant v-Src
Product competes with ATP.
Reversible: yes
Target IC50: 1.5 nM against I338G mutant v-Src; 1.0 µM against wild-type v-Src; 600 nM against wild-type Fyn
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, refrigerate (4°C). Stock solutions are stable for up to 3 months at 4°C.
Other Notes
Bishop, A.C., et al. 2000. Nature407, 395.
Bishop, A.C., et al. 1999 J. Am. Chem. Soc.121, 627.
Bishop, A.C., et al. 1999 J. Am. Chem. Soc.121, 627.
Legal Information
Not available for sale in the United States.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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KangBo Ng et al.
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Engineered analog sensitive kinases provide a highly effective method for acute, controllable, and highly selective inhibition of kinase activity. Here we describe the design and characterization of an analog sensitive allele of the polarity kinase, PKC-3. This allele supports normal
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The generation of distinct cell fates during development depends on asymmetric cell division of progenitor cells. In the central and peripheral nervous system of Drosophila, progenitor cells respectively called neuroblasts or sensory organ precursors use PAR polarity during mitosis to
KangBo Ng et al.
Current biology : CB, 33(20), 4298-4311 (2023-09-21)
During development, the conserved PAR polarity network is continuously redeployed, requiring that it adapt to changing cellular contexts and environmental cues. In the early C. elegans embryo, polarity shifts from being a cell-autonomous process in the zygote to one that must
Mai Usui et al.
Genes to cells : devoted to molecular & cellular mechanisms, 21(4), 302-310 (2016-01-27)
Brown adipocytes and beige adipocytes can expend energy, generate heat, and increase whole-body energy expenditure. The detailed mechanisms of adipogenesis and thermogenesis of these cells are still obscure. Here, we show that Src family kinases (SFKs) regulate both brown adipogenesis
M Ivars et al.
The British journal of dermatology, 182(5), 1194-1204 (2019-08-02)
Acantholysis in pemphigus vulgaris (PV) may be triggered by desmoglein (Dsg) and non-Dsg autoantibodies. The autoantibody profile of each patient results in distinct intracellular signalling patterns. Based on our previous findings, we aimed to elucidate whether PV acantholysis in a
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