PP2 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

The Src family of non-receptor tyrosine kinases regulate cell adhesion, growth, and differentiation through activation of multiple intracellular signaling pathways. Normally inactive, Src kinases are transiently activated during mitosis and constitutively activated by abnormal mutations. PP2 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. It inhibits p56^lck (IC₅₀ = 4 nM), p59^fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM), and Src (IC₅₀ = 100 nM). PP2 does not significantly affect the activity of EGFR kinase (IC₅₀ = 480 nM), JAK2 (IC₅₀ > 50 μM), or ZAP-70 (IC₅₀ > 100 μM). PP2 inhibits the activation of focal adhesion kinase as well as its phosphorylation at Tyr⁵⁷⁷. PP2 also inhibits anti-CD3-stimulated tyrosine phosphorylation of human T-cells with an IC₅₀ value of 600 nM.

Verwenden

PP2 has been used:

• to analyze the effects of Src/focal adhesion kinase (FAK) signaling on IQ domain GTPase-activating protein 1 (IQGAP1)-mediated anoikis resistance
• for Src inhibition to study its effect on epidermal growth factor receptor (EGFR) and nuclear factor erythroid 2-related factor 2 (Nrf2) phosphorylation in non-small cell lung cancer (NSCLC) cells
• for pharmacological inhibition of SRC in MDA-MB-231 breast cancer cells

Biologische Aktivit?t

Selective inhibitor of Src-family tyrosine kinases. Inhibits p56 lck and p59 fynT (IC 50 values are 4 and 5 nM respectively). Displays > 10000-fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC 50 = 0.73 μ M).

Enzyminhibitor

This cell-permeable and photosensitive ATP site-directed pyrazolepyrimidine (FW = 301.78 g/mol), also known as 4-amino-5-(4- chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine and tyrphostin AG 1879, potently inhibits Lck and Fyn protein kinases, with IC50 values of 4 nM and 5 nM. PP2 is ~100x less potent toward EGFR and is inactive for ZAP-70, JAK2 and PKA. PP2 prevented serum-independent growth of RET/PTC1-transformed NIH3T3 fibroblasts and of TPC1 and FB2, two human papillary thyroid carcinoma cell lines that carry spontaneous RET/PTC1 rearrangements. PP2 activates the E-cadherin-mediated cell adhesion system, suppressing metastasis in cancer cells. In cervical cancer cells (HeLa and SiHa), 10 μM PP2 down-regulates pSrc-Y416, pEGFR-Y845, and pEGFR-Y1173 expression levels, while downregulatING pSrc-Y416 and pEGFR-Y845, but not pEGFR-Y1173. PP2 is also a potential neuroprotective agent in cerebral ischemia-reperfusion. Target(s): casein kinase 1d, IC50 = 1.3 μM; Csk protein-tyrosine kinase; focal adhesion kinase; lymphocyte kinase, IC50 = 0.06 μM; p56lck, IC50 = 4 nM; p59fynT, IC50 = 5 nM; receptor proteintyrosine kinase; src protein-tyrosine kinase, IC50 = 0.7 μM (5,11,12- 23); stress-activated protein kinase 2a/p38, IC50 = 1.4 μM; and Yes kinase.

PP2 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

PP2 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Shanghai Daken Advanced Materials Co.,Ltd	+86-2158073036	info@dakenam.com	China	14014	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	33024	60
Alchem Pharmtech,Inc.	8485655694	sales@alchempharmtech.com	United States	63687	58
Shaanxi Dideu Medichem Co. Ltd	+86-29-87569266 +86-17392581500	1015@dideu.com	China	3991	58
Neostar United (Changzhou) Industrial Co., Ltd.	+86-0519-85551759 +8613506123987	marketing1@neostarunited.com	China	8828	58
TargetMol Chemicals Inc.	+1-781-999-5354; +17819995354	marketing@targetmol.com	United States	32467	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6312	58
BOC Sciences	16314854226; +16314854226	inquiry@bocsci.com	United States	19853	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6391	58
HANGZHOU LEAP CHEM CO., LTD.	+86-571-87711850	market18@leapchem.com	China	24597	58

172889-27-9()Verwandte Suche:

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• [1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-yl]amine
• 1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine
• PP2(AG 1879)
• AGL 1879
• PP 2 (enzyme inhibitor)
• Src kinase inhibitor PP2
• 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-
• AG 1879,AGL 1879
• 3-(4-Chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine AGL 1879
• 4-Amino-3-(4-chlorophenyl)-1-(t-butyl)-1H-pyrazolo[3,4-d]pyrimidine
• PP2;AGL 1879;PP 2;PP-2
• 1-(TERT-BUTYL)-3-(4-CHLOROPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE
• 1-(TERT-BUTYL)-3-(4-CHLOROPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE
• 3-(4-CHLOROPHENYL) 1-(1,1-DIMETHYLETHYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE
• 4-AMINO-5-(4-CHLOROPHENYL)-7-(T-BUTYL)PYRAZOLO[3,4-D]PYRIMIDINE
• 4-AMINO-5-(4-CHLOROPHENYL)-7-(TERT-BUTYL)PYRAZOLO[3,4-D]PYRIMIDINE
• AG 1879
• 3-(4-Chlorophenyl)-1-(1,1-dimethylethyl)-(1H)-pyrazolo[3.4-d]pyrimidine-4-amine
• PP2
• PP 2;AG1879;AG 1879;AGL 1879
• PP2(AGL 1879)
• CS-717
• 7-tert-butyl-5-(4-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
• Src family kinase inhibitor PP2
• PP2, Src and RIP2 kinase inhibitor
• PP2, 10 mM in DMSO
• 172889-27-9
• C15H16ClN5
• Inhibitors
• Protein Kinase
• Signalling