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Merck

529573

PP2

≥95% (HPLC), solid, Src protein tyrosine kinase inhibitor, Calbiochem®

別名:

PP2, AG 1879, 4-Amino-5-(4-chlorophenyl)-7-( t-butyl)pyrazolo[3,4-d]pyrimidine

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この商品について

実験式（ヒル表記法）:
C15H16ClN5
CAS番号:
172889-27-9
分子量:
301.77
MDL number:
MFCD01568210
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze

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製品名

PP2, PP2, CAS 172889-27-9, is a potent, reversible, ATP-competitive, inhibitor of the Src family of protein tyrosine kinases (IC50 = 4, 5, 5, &100 nM for p56lck, p59fynT, Hck, & Src, respectively).

SMILES string

Clc1ccc(cc1)c2n[n](c3ncnc(c32)N)C(C)(C)C

InChI

1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)

InChI key

PBBRWFOVCUAONR-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

off-white

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

関連するカテゴリー

General description

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. Inhibits p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM), and Src (IC50 = 100 nM). Does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 >50 µM), or ZAP-70 (IC50 >100 µM). Inhibits the activation of focal adhesion kinase and its phosphorylation at Tyr577. Also potently inhibits anti-CD3-stimulated tyrosine phosphorylation of human T cells (IC50 = 600 nM). A 10 mM (1 mg/331 µl) solution of PP2 (Cat. No. 529576) in DMSO also available.

Biochem/physiol Actions

Cell permeable: no
Primary Target
p56lck
Product competes with ATP.
Reversible: yes
Target IC50: 4 nM, 5 nM, 5 nM, 100 nM, against p56lck, p59fynT, Hck, and Src, respectively; 600 nM against anti-CD3-stimulated tyrosine phosphorylation of human T cells

Packaging

Packaged under inert gas

Preparation Note

Further dilute with aqueous buffers just prior to use.

Other Notes

Karni, R., et al. 2003. FEBS Lett.537, 47.
Salazar, E.P., and Rozengurt, E. 1999. J. Biol. Chem. 274, 28371.
Hanke, J.H., et al. 1996. J. Biol. Chem.271, 695.



Selected Citations
Lee, J., et al. 2009. Cell Stem Cell5, 76.


Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

wgk

WGK 3

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

529573-5MG: + 529573-30MG: + 529573-VMG: + 529573-1MG: + 529573-50MG:

jan

試験成績書（COA）

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以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

Yuko Murakami-Nishimagi et al.
Breast cancer research : BCR, 25(1), 41-41 (2023-04-15)
Cell adhesion is indispensable for appropriate tissue architecture and function in multicellular organisms. Besides maintaining tissue integrity, cell adhesion molecules, including tight-junction proteins claudins (CLDNs), exhibit the signaling abilities to control a variety of physiological and pathological processes. However, it
Quanri Zhang et al.
Experimental & molecular medicine, 50(2), e439-e439 (2018-02-06)
During mycobacteria infection, anti-inflammatory responses allow the host to avoid tissue damage caused by overactivation of the immune system; however, little is known about the negative modulators that specifically control mycobacteria-induced immune responses. Here we demonstrate that integrin CD11b is
Elliot Dine et al.
Cell reports, 35(12), 109280-109280 (2021-06-24)
Protein clustering is pervasive in cell signaling, yet how signaling from higher-order assemblies differs from simpler forms of molecular organization is still poorly understood. We present an optogenetic approach to switch between oligomers and heterodimers with a single point mutation.
Emily C Suter et al.
Cell reports, 36(8), 109587-109587 (2021-08-26)
Cancer immunotherapies often modulate macrophage effector function by introducing either targeting antibodies that activate Fcγ receptors (FcγRs) or blocking antibodies that disrupt inhibitory SIRPα-CD47 engagement. However, how these competing signals are integrated is poorly understood, raising questions about how to
Zahra Alvandi et al.
Methods in molecular biology (Clifton, N.J.), 2520, 261-264 (2021-10-07)
Embryonic stem cells (ESCs) are a unique model that allows the study of molecular pathways underlying commitment and differentiation. We have studied signaling pathways and their contributions to osteogenic differentiation. In addition to our previously published protocol where we recommended
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関連コンテンツ

An Introduction to Inhibitors and Their Biological Applications - 1st Edition

An Introduction to Inhibitors and Their Biological Applications

Fluorescent Gelatin Degradation Assays for Investigating Invadopodia Formation

QCM™ Gelatin Invadopodia Assays provide optimized materials and protocols to enable reproducible analysis of invadopodia in invasive tumor cells (Catalog No. ECM670 for green fluorescence, Catalogue No. ECM671 for red fluorescence). Reagents are provided for coating glass culture surfaces with fluorescent matrix and for colocalizing the actin cytoskeleton and nuclei with invadopodial degradation sites. This assay may also be used for assessing the activity of inhibitors and promoters of invadopodia formation and function. Furthermore, different cell types and individual cells in heterogeneous populations may be analyzed for invasive potential. Finally, the assay kits provide troubleshooting suggestions, recommendations for coating on multiple substrate formats, and example studies in several assay systems (e.g., various cell types, time-course studies, degradation modulation).

Bulk Product Guide
Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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グローバルトレードアイテム番号

カタログ番号GTIN
529573-1MGCN07790788051198
529573-5MGCN04055977269802

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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