PP2
- Product Name
- PP2
- CAS No.
- 172889-27-9
- Chemical Name
- PP2
- Synonyms
- PP2;CS-717;AG 1879;AGL 1879;PP2(AG 1879);PP2(AGL 1879);AG 1879,AGL 1879;PP2;AGL 1879;PP 2;PP-2;PP 2 (enzyme inhibitor);Src kinase inhibitor PP2
- CBNumber
- CB1406580
- Molecular Formula
- C15H16ClN5
- Formula Weight
- 301.77
- MOL File
- 172889-27-9.mol
PP2 Property
- Boiling point:
- 493.5±40.0 °C(Predicted)
- Density
- 1.35±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 3 mg/ml with warming).
- form
- Off-white solid
- pka
- 3.96±0.30(Predicted)
- color
- Off-white
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
N-Bromosuccinimide Price
- Product number
- 529573
- Product name
- PP2
- Packaging
- 1mg
- Price
- $159
- Updated
- 2024/03/01
- Product number
- P0042
- Product name
- PP2
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $201
- Updated
- 2024/03/01
- Product number
- 529573
- Product name
- PP2
- Packaging
- 5mg
- Price
- $303
- Updated
- 2024/03/01
- Product number
- 13198
- Product name
- PP2
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 13198
- Product name
- PP2
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $70
- Updated
- 2024/03/01
PP2 Chemical Properties,Usage,Production
Description
The Src family of non-
Uses
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
Definition
ChEBI: PP2 is a member of the class of pyrazolopyrimidine that is pyrazolo[3,4-d]pyrimidin-4-amine bearing additional tert-butyl and 4-chlorophenyl substituents at positions 1 and 3 respectively. It is a potent ATP-competitive inhibitor of the Src family of protein tyrosine kinases. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, a beta-adrenergic antagonist and a geroprotector. It is a pyrazolopyrimidine, an aromatic amine and a member of monochlorobenzenes.
Biological Activity
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).
Biochem/physiol Actions
PP2 is a selective inhibitor of Src-family tyrosine kinases of non-receptor tyrosine kinases (nRTK). It shows >10,000-fold selectivity over Zeta-chain-associated protein kinase 70 (ZAP-70) and Janus kinase 2 (JAK2). PP2 effectively reduces cervical cancer proliferation in vitro and in vivo.
Enzyme inhibitor
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.
storage
+4°C (desiccate)
References
1) Hanke et al. (1996), Discovery of a novel, potent and Src family-selective kinase inhibitor. Study of Lck-and FynT-dependent T cell activation; J. Biol. Chem., 271 695 2) Yoshizume et al. (2000), Src and Cas mediate JNK activation but not ERK1/2 and p38 kinases by reactive oxygen species; J. Biol. Chem., 275 11706
PP2 Preparation Products And Raw materials
Raw materials
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