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Merck

529579

PP1 Analog

Synonym(s):

PP1 Analog, 4-Amino-1- tert-butyl-3-(1ʹ-naphthyl)pyrazolo[3,4-d]pyrimidine, 1-Na PP1, 1-NA-PP1

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About This Item

Empirical Formula (Hill Notation):
C19H19N5
CAS Number:
Molecular Weight:
317.39
UNSPSC Code:
12352202
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InChI key

XSHQBIXMLULFEV-UHFFFAOYSA-N

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)

assay

≥99% (HPLC)

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

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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

Disclaimer

Toxicity: Standard Handling (A)

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).

Legal Information

Not available for sale in the United States.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Bishop, A.C., et al. 2000. Nature407, 395.
Bishop, A.C., et al. 1999 J. Am. Chem. Soc.121, 627.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, refrigerate (4°C). Stock solutions are stable for up to 3 months at 4°C.

Storage Class

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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Nicolas Loyer et al.
eLife, 13 (2024-06-13)
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
KangBo Ng et al.
microPublication biology, 2022 (2022-08-24)
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
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
Jinlong Wang et al.
Cell, 185(17), 3186-3200 (2022-07-31)
Upon stress, eukaryotes typically reprogram their translatome through GCN2-mediated phosphorylation of the eukaryotic translation initiation factor, eIF2α, to inhibit general translation initiation while selectively translating essential stress regulators. Unexpectedly, in plants, pattern-triggered immunity (PTI) and response to other environmental stresses

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